328 articles for thisTarget
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Computational studies on HIV-1 protease inhibitors: influence of calculated inhibitor-enzyme binding affinities on the statistical quality of 3D-QSAR CoMFA models.
University Of Missouri St. Louis
Comparative binding energy analysis of HIV-1 protease inhibitors: incorporation of solvent effects and validation as a powerful tool in receptor-based drug design.
Universidad De Alcal£
Hydrophobicity in the design of P2/P2' tetrahydropyrimidinone HIV protease inhibitors.
Clarkson University
DoMCoSAR: a novel approach for establishing the docking mode that is consistent with the structure-activity relationship. Application to HIV-1 protease inhibitors and VEGF receptor tyrosine kinase inhibitors.
Eli Lilly
3D-quantitative structure-activity relationships of human immunodeficiency virus type-1 proteinase inhibitors: comparative molecular field analysis of 2-heterosubstituted statine derivatives-implications for the design of novel inhibitors.
Sandoz Forschungsinstitut Ges.M.B.H.
Three-dimensional quantitative structure-activity relationship of human immunodeficiency virus (I) protease inhibitors. 2. Predictive power using limited exploration of alternate binding modes.
Washington University
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 4. 3-[2-(Benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one and analogues.
Merck Reserch Laboratories
Three-dimensional QSAR of human immunodeficiency virus (I) protease inhibitors. 1. A CoMFA study employing experimentally-determined alignment rules.
Washington University
Six-membered cyclic ureas as HIV-1 protease inhibitors: a QSAR study based on CODESSA PRO approach. Quantitative structure-activity relationships.
University Of Florida
Synthesis and antiviral activity of a novel class of HIV-1 protease inhibitors containing a heterocyclic P1-P2 amide bond isostere
TBA
Stereocontrolled synthesis and biological activity of two diastereoisomers of the potent HIV-1 protease inhibitor saquinavir.
Sapienza University Of Rome
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385.
Glaxosmithkline
Microwave-accelerated synthesis of P1'-extended HIV-1 protease inhibitors encompassing a tertiary alcohol in the transition-state mimicking scaffold.
Uppsala University
Development of low molecular weight HIV-1 protease dimerization inhibitors.
Purdue University
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
Uppsala University
A unidirectional crosslinking strategy for HIV-1 protease dimerization inhibitors.
Purdue University
A phenylnorstatine inhibitor binding to HIV-1 protease: geometry, protonation, and subsite-pocket interactions analyzed at atomic resolution.
Academy Of Sciences Of The Czech Republic
Countering cooperative effects in protease inhibitors using constrained beta-strand-mimicking templates in focused combinatorial libraries.
The University Of Queensland
Dimerization inhibitors of HIV-1 protease based on a bicyclic guanidinium subunit.
Universidad Aut£Noma De Madrid
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.
Uppsala University
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
Universita' Degli Studi Di Salerno
4-Hydroxy-5,6-dihydropyrones as inhibitors of HIV protease: the effect of heterocyclic substituents at C-6 on antiviral potency and pharmacokinetic parameters.
Pfizer
Conformational selection of inhibitors and substrates by proteolytic enzymes: implications for drug design and polypeptide processing.
University Of Queensland
Synthesis, stability, antiviral activity, and protease-bound structures of substrate-mimicking constrained macrocyclic inhibitors of HIV-1 protease.
The University Of Queensland
Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.
Merck Research Laboratories
Modeling of the inhibition of retroviral integrases by styrylquinoline derivatives.
Cnrs Umr 8532
Optimizing the binding of fullerene inhibitors of the HIV-1 protease through predicted increases in hydrophobic desolvation.
University Of California
Viracept (nelfinavir mesylate, AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease.
Agouron Pharmaceuticals
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.
University Of Pennsylvania
Antiretroviral agents as inhibitors of both human immunodeficiency virus type 1 integrase and protease.
National Cancer Institute-Bethesda
Application of the three-dimensional structures of protein target molecules in structure-based drug design.
Abbott Laboratories
Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: biotinylated HIV-1 protease inhibitors.
Upjohn Laboratories
Inhibitors of the protease from human immunodeficiency virus: synthesis, enzyme inhibition, and antiviral activity of a series of compounds containing the dihydroxyethylene transition-state isostere.
Upjohn Laboratories
Peptidomimetic HIV protease inhibitors: phosphate prodrugs with improved biological activities.
Upjohn
Multiple copy simultaneous search and construction of ligands in binding sites: application to inhibitors of HIV-1 aspartic proteinase.
Harvard University
Intriguing structure-activity relations underlie the potent inhibition of HIV protease by norstatine-based peptides.
Syntex Research
New hydroxyethylamine HIV protease inhibitors that suppress viral replication.
University Of Wisconsin-Madison
Inhibitors of the protease from human immunodeficiency virus: design and modeling of a compound containing a dihydroxyethylene isostere insert with high binding affinity and effective antiviral activity.
Upjohn
HIV protease: a novel chemotherapeutic target for AIDS.
Merck Sharp And Dohme Research Laboratories
Examination of HIV-1 protease secondary structure specificity using conformationally constrained inhibitors.
University Of Illinois
Novel binding mode of highly potent HIV-proteinase inhibitors incorporating the (R)-hydroxyethylamine isostere.
Roche Products
Structure-based design and synthesis of HIV-1 protease inhibitors employing beta-D-mannopyranoside scaffolds.
University College Dublin
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
Dupont Pharmaceuticals
Simplified catechin-gallate inhibitors of HIV-1 reverse transcriptase.
University Of Toledo
Design and synthesis of new inhibitors of HIV-1 protease dimerization with conformationally constrained templates.
Kyoto Pharmaceutical University
The sulfonimidamide as a novel transition state analog for aspartic acid and metallo proteases.
The University Of Kansas
Structure based design: novel spirocyclic ethers as nonpeptidal P2-ligands for HIV protease inhibitors.
University Of Illinois At Chicago
Restricting the flexibility of crosslinked, interfacial peptide inhibitors of HIV-1 protease.
Purdue University
Peptidomimetic inhibitors of human immunodeficiency virus protease (HIV-PR): Design, enzyme binding and selectivity, antiviral efficacy, and cell permeability properties
TBA
Synthesis of irreversible HIV-1 protease inhibitors containing sulfonamide and sulfone as amide bond isosteres
TBA
Cyclic urea HIV protease inhibitors containing alkynyl- and alkenyl-tethered heterocycles in the P2 region
TBA
Design, synthesis, and characterization of dipeptide isostere containing cis-epoxide for the irreversible inactivation of HIV protease
TBA
β-Methanesulfonyl-L-valine as a novel, unnatural amino acid surrogate for P2 in the design of HIV protease inhibitors.
TBA
(Hydroxyethyl) sulfonamide HIV-1 Protease inhibitors: Identification of the 2-methylbenzoyl moiety at P-2
TBA
Synthesis and activity of conformationally-constrained macrocyclic norstatine-based inhibitors of HIV protease
TBA
Nonpeptidic HIV protease inhibitors: 3-(S-benzyl substituted)-4-hydroxy-6-(phenyl substituted)-2H-pyran-2-one with an inverse mode of binding
TBA
A topliss tree analysis of the HIV-protease inhibitory activity of 6-phenyl-4-hydroxy-pyran-2-ones
TBA
Aminodiol HIV protease inhibitors. 2. 1,1-Dimethyl-2-hydroxyethyl carbamate derivatives with enhanced potency
TBA
Ly316340: A potent HIV-1 protease inhibitor containing a high affinity octahydrothienopyridine hydroxyethylamine isostere
TBA
Evaluation of substituted benzamides as P2 ligands for symmetry-based inhibitors of HIV protease
TBA
Structure-based design of achiral anthranilamides as P2/P2′ surrogates for symmetry-based HIV protease inhibitors: design, synthesis, X-ray structure, enzyme inhibition and antiviral activity
TBA
Thiophene derivatives as extremely high affinity P3′ ligands for the hydroxyethylpiperazine class of HIV-1 protease inhibitors
TBA
Substituted alkylpyridines as P3′ ligands for the hydroxyethylpiperazine class of HIV-1 protease inhibitors: Improved pharmacokinetic profiles
TBA
Symmetry-based HIV Protease inhibitors: rational design of 2-methylbenzamides as novel P2/P2′ ligands
TBA
Cyclic sulfone-3-carboxamides as novel P2-ligands for Ro 31-8959 based HIV-1 protease inhibitors
TBA
Synthesis of C2-symmetric inhibitors of the HIV-1 protease, with N,N′-substituted ethylenediamide and ethylenediamine linkers.
TBA
Design, structure activity and x-ray crystallographic studies of pseudosymmetrical nonpeptidyl HIV-1 protease inhibitors
TBA
Novel, extended transition state mimic in HIV-1 protease inhibitors with peripheral C-2-symmetry
TBA
Beneficial replacement of the P1 phenylalanine side chain in HIV-1 protease inhibitors of the difluorostatone type
TBA
A new hydroxyethylamine class of HIV-1 protease inhibitors with high antiviral potency and oral bioavailability
TBA
Design, synthesis, and activity of conformationally-constrained macrocyclic peptide-based inhibitors of HIV protease
TBA
Novel conformationally constrained HIV-1 protease inhibitors: rational design, enzyme inhibition, and X-ray structure of an enzyme-inhibtor complex
TBA
Increased antiviral activity of HIV protease inhibitors of the difluorostatone type bearing (R)-valinol derivatives as novel c-termini
TBA
Inhibition of human immunodeficiency virus-1 protease by a C2-symmetrical phosphinic acid amide
TBA
Difunctional enols of N-protected amino acids as low molecular weight and novel inhibitors of HIV-1 protease.
TBA
Novel dimeric penicillin derived inhibitors of HIV-1 proteinase: interaction with the catalytic aspartates
TBA
Rapid discovery and structure-activity profiling of novel inhibitors of human immunodeficiency virus type 1 protease enabled by the copper(I)-catalyzed synthesis of 1,2,3-triazoles and their further functionalization.
The Scripps Research Institute
HIV-1 protease mutations and inhibitor modifications monitored on a series of complexes. Structural basis for the effect of the A71V mutation on the active site.
Academy Of Sciences Of The Czech Republic
Molecular tongs containing amino acid mimetic fragments: new inhibitors of wild-type and mutated HIV-1 protease dimerization.
Paris-Sud University
A new class of HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold.
Uppsala University
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains.
Abbott Laboratories
Design, synthesis, and biological evaluation of novel 4-hydroxypyrone derivatives as HIV-1 protease inhibitors.
Peking University
Beta-lactam compounds as apparently uncompetitive inhibitors of HIV-1 protease.
University Of Debrecen
New 2-bromomethyl-8-substituted-benzo[c]chromen-6-ones. Synthesis and biological properties.
University Of The Mediterranean
New constrained"molecular tongs" designed to dissociate HIV-1 protease dimer.
Paris-Sud University
Efficient evaluation of binding free energy using continuum electrostatics solvation.
University Of ZüRich
Facile incorporation of urea pseudopeptides into protease substrate analogue inhibitors.
Purdue University
Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors.
Abbott Laboratories
Novel nonpeptidic inhibitors of HIV-1 protease obtained via a new multicomponent chemistry strategy.
Morphochem
BREED: Generating novel inhibitors through hybridization of known ligands. Application to CDK2, p38, and HIV protease.
Vertex Pharmaceuticals
Design and evaluation of novel piperidine HIV-1 protease inhibitors with potency against DRV-resistant variants.
Chinese Academy Of Medical Science And Peking Union Medical College
Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase.
Chinese Academy Of Medical Science And Peking Union Medical College
l-2',3'-Didehydro-2',3'-dideoxy-3'-fluoronucleosides: synthesis, anti-HIV activity, chemical and enzymatic stability, and mechanism of resistance.
The University Of Georgia
Design and synthesis of highly potent HIV protease inhibitors with activity against resistant virus.
Merck Research Laboratories
Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains.
Kyoto University
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
University Of Nebraska Medical Center
Synthesis, antiviral activity and pharmacokinetics of P1/P1' substituted 3-aminoindazole cyclic urea HIV protease inhibitors.
Bristol-Myers Squibb
Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities.
Purdue University
Design and synthesis of pseudo-symmetric HIV protease inhibitors containing a novel hydroxymethylcarbonyl (HMC)-hydrazide isostere.
Kyoto Pharmaceutical University
Combinatorial library of indinavir analogues: replacement for the aminoindanol at P2'.
Merck Research Laboratories
Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains.
Merck Research Laboratories
Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.
Merck Research Laboratories
Synthesis and antiviral activity of new anti-HIV amprenavir bioisosteres.
University Of The Mediterranean
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.
Pfizer
Rational design and Structure-Activity relationship of coumarin derivatives effective on HIV-1 protease and partially on HIV-1 reverse transcriptase.
Chinese Academy Of Medical Science And Peking Union Medical College
A combinatorial library of indinavir analogues and its in vitro and in vivo studies.
Merck Research Laboratories
Elucidating the inhibiting mode of AHPBA derivatives against HIV-1 protease and building predictive 3D-QSAR models.
Chinese Academy Of Sciences
Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere.
University Of Massachusetts Medical School
Design and biological evaluation of novel HIV-1 protease inhibitors with isopropanol as P1' ligand to enhance binding with S1' subsite.
Chinese Academy Of Medical Science And Peking Union Medical College
Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir).
Abbott Laboratories
Novel HIV-1 Protease Inhibitors with Morpholine as the P2 Ligand to Enhance Activity against DRV-Resistant Variants.
Chinese Academy Of Medical Science And Peking Union Medical College
Design, synthesis and biological evaluation of HIV-1 protease inhibitors with morpholine derivatives as P2 ligands in combination with cyclopropyl as P1' ligand.
Jinzhou Medical University
Design, synthesis, and biological evaluation of HIV/FIV protease inhibitors incorporating a conformationally constrained macrocycle with a small P3' residue.
The Scripps Research Institute
6-Hydroxy-1,3-dioxin-4-ones as non-peptidic HIV protease inhibitors.
Institute Of Science & Technology
Use of proline bioisosteres in potential HIV protease inhibitors: phenylalanine-2-thiophenoxy-3-pyrrolidinone: synthesis and anti-HIV evaluation.
Université
Combinatorial diversification of indinavir: in vivo mixture dosing of an HIV protease inhibitor library.
Merck Research Laboratories
'Double-Drugs'--a new class of prodrug form of an HIV protease inhibitor conjugated with a reverse transcriptase inhibitor by a spontaneously cleavable linker.
Kyoto Pharmaceutical University
A new class of HIV-1 integrase inhibitors: the 3,3,3', 3'-tetramethyl-1,1'-spirobi(indan)-5,5',6,6'-tetrol family.
University Of California
Synthesis and biological evaluation of the first N-alkyl cage dimeric 4-aryl-1,4-dihydropyridines as novel nonpeptidic HIV-1 protease inhibitors.
Martin-Luther-University Halle-Wittenberg
Unsymmetrical cyclic ureas as HIV-1 protease inhibitors: novel biaryl indazoles as P2/P2' substituents.
Dupont Pharmaceuticals
Inhibitors of the C(2)-symmetric HIV-1 protease: nonsymmetric binding of a symmetric cyclic sulfamide with ketoxime groups in the P2/P2' side chains.
Uppsala University
Increased antiviral activity of cyclic urea HIV protease inhibitors by modifying the P1/P1' substituents.
Dupont Pharmaceuticals
4-hydroxy-5,6-dihydro-2H-pyran-2-ones.3. Bicyclic and hetero-aromatic ring systems as 3-position scaffolds to bind to S1' and S2' of the HIV-1 protease enzyme.
Warner-Lambert
Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl,5-methylphenyl thio) moiety: antiviral activities and pharmacokinetic properties.
Warner-Lambert
Structure-based design of diaminopyranosides as a novel inhibitor core unit of HIV proteases.
Biomolecular Engineering Research Institute
A new class of anti-HIV agents: synthesis and activity of conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor.
Kyoto Pharmaceutical University
Design, synthesis, and evaluation of conformationally constrained tongs, new inhibitors of HIV-1 protease dimerization.
Université
Design and synthesis of novel conformationally restricted HIV protease inhibitors.
Vertex Pharmaceuticals
Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors.
Vertex Pharmaceuticals
Unsymmetric nonpeptidic HIV protease inhibitors containing anthranilamide as a P2' ligand.
Aids Drug Screening And Development Laboratory
Three-dimensional quantitative structure-activity relationship study on cyclic urea derivatives as HIV-1 protease inhibitors: application of comparative molecular field analysis.
Lindsley F. Kimball Research Institute
NMR and topochemical studies of peptidomimetic HIV-I protease inhibitors containing a cis-epoxide amide isostere.
Biotech Research Institute
Synthesis and anti-HIV activities of symmetrical N1,N3-dibenzyl-2-hydroxy-propane derivatives.
Université
Non-peptidic HIV protease inhibitors: C2-symmetry-based design of bis-sulfonamide dihydropyrones.
Pharmacia & Upjohn
The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: modifications of the P1/P1' residues.
Dupont Pharmaceuticals
Potent cyclic urea HIV protease inhibitors with 3-aminoindazole P2/P2' groups.
Dupont Pharmaceuticals
Novel HIV-protease inhibitors containing beta-hydroxyether and -thioether dipeptide isostere surrogates: modification of the P3 ligand.
Schering-Plough Research Institute
Design and synthesis of new potent C2-symmetric HIV-1 protease inhibitors. Use of L-mannaric acid as a peptidomimetic scaffold.
LinköPing University
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues.
Dupont Pharmaceuticals
Cyclic HIV protease inhibitors: design and synthesis of orally bioavailable, pyrazole P2/P2' cyclic ureas with improved potency.
Dupont Pharmaceuticals
Cyclopropane-derived peptidomimetics. Design, synthesis, evaluation, and structure of novel HIV-1 protease inhibitors.
National Cancer Institute-Frederick
Discovery of ritonavir, a potent inhibitor of HIV protease with high oral bioavailability and clinical efficacy.
Abbott Laboratories
Cyclic urea amides: HIV-1 protease inhibitors with low nanomolar potency against both wild type and protease inhibitor resistant mutants of HIV.
Dupont Pharmaceuticals
Structure-based design of HIV protease inhibitors: 5,6-dihydro-4-hydroxy-2-pyrones as effective, nonpeptidic inhibitors.
Pharmacia & Upjohn
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Dupont Pharmaceuticals
Cycloalkylpyranones and cycloalkyldihydropyrones as HIV protease inhibitors: exploring the impact of ring size on structure-activity relationships.
Pharmacia And Upjohn
New series of potent, orally bioavailable, non-peptidic cyclic sulfones as HIV-1 protease inhibitors.
Gilead Sciences
Pyrrolobenzothiazepinones and pyrrolobenzoxazepinones: novel and specific non-nucleoside HIV-1 reverse transcriptase inhibitors with antiviral activity.
Universitá
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents.
University Of North Carolina At Chapel Hill
Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers.
Medichem Research
Symmetry-based inhibitors of HIV protease. Structure-activity studies of acylated 2,4-diamino-1,5-diphenyl-3-hydroxypentane and 2,5-diamino-1,6-diphenylhexane-3,4-diol.
Abbott Laboratories
A novel constrained reduced-amide inhibitor of HIV-1 protease derived from the sequential incorporation of gamma-turn mimetics into a model substrate.
Smithkline Beecham Pharmaceuticals
A series of penicillin-derived C2-symmetric inhibitors of HIV-1 proteinase: structural and modeling studies.
Glaxo Group Research
Calculation of relative differences in the binding free energies of HIV1 protease inhibitors: a thermodynamic cycle perturbation approach.
Agouron Pharmaceuticals
Haloperidol-based irreversible inhibitors of the HIV-1 and HIV-2 proteases.
University Of California
Structure-based design of HIV-1 protease inhibitors: replacement of two amides and a 10 pi-aromatic system by a fused bis-tetrahydrofuran.
Merck Research Laboratories
Synthesis and structure-activity relationships of a series of penicillin-derived HIV proteinase inhibitors: heterocyclic ring systems containing P1' and P2' substituents.
Glaxo Research And Development
Design, synthesis, and conformational analysis of a novel macrocyclic HIV-protease inhibitor.
Marion Merrell Dow Research Institute
L-735,524: the design of a potent and orally bioavailable HIV protease inhibitor.
Merck Research Laboratories
Rational design, synthesis, and crystallographic analysis of a hydroxyethylene-based HIV-1 protease inhibitor containing a heterocyclic P1'--P2' amide bond isostere.
Smithkline Beecham Pharmaceuticals
Inhibitors of HIV-1 protease containing the novel and potent (R)-(hydroxyethyl)sulfonamide isostere.
Searle Discovery Research
Cosalane analogues with enhanced potencies as inhibitors of HIV-1 protease and integrase.
Purdue University
A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site.
Merck Research Laboratories
A check on rational drug design: crystal structure of a complex of human immunodeficiency virus type 1 protease with a novel gamma-turn mimetic inhibitor.
Smithkline Beecham Pharmaceuticals
Synthetic chemical diversity: solid phase synthesis of libraries of C2 symmetric inhibitors of HIV protease containing diamino diol and diamino alcohol cores.
Abbott Laboratories
Anti-AIDS (acquired immune deficiency syndrome) agents. 17. New brominated hexahydroxybiphenyl derivatives as potent anti-HIV agents.
University Of North Carolina At Chapel Hill
Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors.
Tosoh
Synthesis of naphthalenesulfonic acid small molecules as selective inhibitors of the DNA polymerase and ribonuclease H activities of HIV-1 reverse transcriptase.
College Of Pharmacy
Structure-based design of nonpeptidic HIV protease inhibitors from a cyclooctylpyranone lead structure.
Upjohn Laboratories
Computational studies on tetrahydropyrimidine-2-one HIV-1 protease inhibitors: improving three-dimensional quantitative structure-activity relationship comparative molecular field analysis models by inclusion of calculated inhibitor- and receptor-based properties.
University Of Missouri-St. Louis
SMall Molecule Growth 2001 (SMoG2001): an improved knowledge-based scoring function for protein-ligand interactions.
Harvard University
6-Biphenylmethyl-3-hydroxypyrimidine-2,4-diones potently and selectively inhibited HIV reverse transcriptase-associated RNase H.
University Of Minnesota
6-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity.
University Of Minnesota
The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation.
Bristol-Myers Squibb Research And Development
Polypharmacology in HIV inhibition: can a drug with simultaneous action against two relevant targets be an alternative to combination therapy?
Instituto De Qu£Mica M£Dica (Iqm, Csic)
Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,1
TBA
Design, synthesis and biological evaluations of N-Hydroxy thienopyrimidine-2,4-diones as inhibitors of HIV reverse transcriptase-associated RNase H.
University Of Minnesota
Hydroxyethylamine analogues of the p17/p24 substrate cleavage site are tight-binding inhibitors of HIV protease.
University Of Wisconsin-Madison
Effect of hydroxyl group configuration in hydroxyethylamine dipeptide isosteres on HIV protease inhibition. Evidence for multiple binding modes.
University Of Wisconsin-Madison
A series of potent HIV-1 protease inhibitors containing a hydroxyethyl secondary amine transition state isostere: synthesis, enzyme inhibition, and antiviral activity.
Merck Research Laboratories
Penicillin derived C2-symmetric dimers as novel inhibitors of HIV-1 proteinase.
Glaxo Group Research
A robust GTP-induced shift in alpha(2)-adrenoceptor agonist affinity in tissue sections from rat brain.
University Of Nebraska
An experimental and molecular-modeling study of the binding of linked sulfated tetracyclitols to FGF-1 and FGF-2.
Progen Industries
A fragment-based approach to understanding inhibition of 1-deoxy-D-xylulose-5-phosphate reductoisomerase.
University Of Bristol
Molecular cloning and expression of the cDNA for the alpha 1A-adrenergic receptor. The gene for which is located on human chromosome 5.
Duke University
Discovery and structure-guided drug design of inhibitors of 11beta-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold.
Merck Serono
Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
Roche Palo Alto
Investigation on the role of the tetrazole in the binding of thiotetrazolylacetanilides with HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases.
Boehringer Ingelheim (Canada)
Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations.
Universita Di Siena
Novel Indazole Non-Nucleoside Reverse Transcriptase Inhibitors Using Molecular Hybridization Based on Crystallographic Overlays (dagger).
Pfizer
Design, Synthesis, Evaluation, and Crystallographic-Based Structural Studies of HIV-1 Protease Inhibitors with Reduced Response to the V82A Mutation.
Universidad De Santiago De Compostela
Pyrazole inhibitors of HMG-CoA reductase: An attempt to dramatically reduce synthetic complexity through minimal analog re-design.
Pfizer
Comparing the accumulation of active- and nonactive-site mutations in the HIV-1 protease.
University Of Florida College Of Medicine
Design of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 1.
University Of Oxford
Synthesis and antiviral activity of 4-benzyl pyridinone derivatives as potent and selective non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors.
Institut Curie
Computational strategies in discovering novel non-nucleoside inhibitors of HIV-1 RT.
Universita Di Messina
Synthesis and antiviral activities of novel N-alkoxy-arylsulfonamide-based HIV protease inhibitors.
Glaxosmithkline
Design and synthesis of potent inhibitors of the malaria aspartyl proteases plasmepsin I and II. Use of solid-phase synthesis to explore novel statine motifs.
Linkoping University
Synthesis of C2 alkynylated purines, a new family of potent inhibitors of cyclin-dependent kinases.
Institut Curie
Pyrazolo[3,4-b]quinoxalines. A new class of cyclin-dependent kinases inhibitors.
Universidad De Navarra
Synthesis and in vitro evaluation of novel 2,6,9-trisubstituted purines acting as cyclin-dependent kinase inhibitors.
Institut Curie
Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.
Avenida De La Industria
Further studies on ethenyl and ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of a subnanomolar Src kinase inhibitor.
Wyeth-Ayerst Research
Inhibitors of src tyrosine kinase: the preparation and structure-activity relationship of 4-anilino-3-cyanoquinolines and 4-anilinoquinazolines.
Wyeth-Ayerst Research
Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides.
Yamanouchi Pharmaceutical
Studies of non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: synthesis and structure-activity relationships of 2-cyano and 2-hydroxy thiazolidenebenzenesulfonamide derivatives.
Yamanouchi Pharmaceutical
Inhibition of wild-type and mutant human immunodeficiency virus type 1 proteases by GW0385 and other arylsulfonamides.
Glaxosmithkline
Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.
Glaxo Group Research
Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one.
Merck Research Laboratories
Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
Merck Research Laboratories
Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.
Dupont Pharmaceuticals
Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors.
Dupont Pharmaceuticals
Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA).
Dupont Pharmaceuticals
Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors.
Dupont Pharmaceuticals
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.
Dupont Pharmaceuticals
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
Dupont Pharmaceuticals
Bioisosteric modification of PETT-HIV-1 RT-inhibitors: synthesis and biological evaluation.
Medivir
Novel modifications in the alkenyldiarylmethane (ADAM) series of non-nucleoside reverse transcriptase inhibitors.
Purdue University
Synthesis of substituted diarylmethylenepiperidines (DAMPs), a novel class of anti-HIV agents.
Purdue University
Synthesis of alkenyldiarylmethane (ADAM) non-nucleoside HIV-1 reverse transcriptase inhibitors with non-identical aromatic rings.
Purdue University
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
Purdue University
New alkenyldiarylmethanes with enhanced potencies as anti-HIV agents which act as non-nucleoside reverse transcriptase inhibitors.
Purdue University
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
Medivir
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C variant.
Sapienza University Of Rome
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.
Sapienza University Of Rome
5H-pyrrolo[1,2-b] [1,2,5]benzothiadiazepines (PBTDs): a novel class of non-nucleoside reverse transcriptase inhibitors.
Sapienza University Of Rome
Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines.
Sapienza University Of Rome
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.
Sapienza University Of Rome
1-[2-(Diphenylmethoxy)ethyl]-2-methyl-5-nitroimidazole: a potent lead for the design of novel NNRTIs.
Sapienza University Of Rome
Synthesis, biological evaluation, and binding mode of novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles targeted at the HIV-1 reverse transcriptase.
Sapienza University Of Rome
Structure-based design, synthesis, and biological evaluation of novel pyrrolyl aryl sulfones: HIV-1 non-nucleoside reverse transcriptase inhibitors active at nanomolar concentrations.
Sapienza University Of Rome
5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives.
Sapienza University Of Rome
2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones.
Universita Di Roma
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Sapienza University Of Rome
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.
Upjohn
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piperazine monomethanesulfonate (U-90152S), a
Upjohn
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Merck Research Laboratories
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.
Merck Sharp And Dohme Research Laboratories
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
Eli Lilly
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.
Upjohn
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
Eli Lilly
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
Glaxosmithkline
Nonpeptide cyclic cyanoguanidines as HIV-1 protease inhibitors: synthesis, structure-activity relationships, and X-ray crystal structure studies.
Dupont Pharmaceuticals
Structure-based design of nonpeptidic HIV protease inhibitors: the sulfonamide-substituted cyclooctylpyramones.
Upjohn
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.
Boehringer Mannheim
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.
Merck Research Laboratories
Design and synthesis of HIV protease inhibitors. Variations of the carboxy terminus of the HIV protease inhibitor L-682,679.
Merck Sharp And Dohme Research Laboratories
Stereospecific synthesis, structure-activity relationship, and oral bioavailability of tetrahydropyrimidin-2-one HIV protease inhibitors.
Dupont Pharmaceuticals
Design, synthesis, and evaluation of tetrahydropyrimidinones as an example of a general approach to nonpeptide HIV protease inhibitors.
Dupont Pharmaceuticals
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1 specific reverse transcriptase inhibitors. 1. Phthalimidoalkyl and -alkylamino analogues.
Merck Research Laboratories
Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class.
Upjohn
A major role for a set of non-active site mutations in the development of HIV-1 protease drug resistance.
The Johns Hopkins University
L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor.
Merck Research Laboratories
Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.
Upjohn