71 articles for thisTarget
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Optimization of P1-P3 groups in symmetric and asymmetric HIV-1 protease inhibitors.
Uppsala University
Bis tertiary amide inhibitors of the HIV-1 protease generated via protein structure-based iterative design.
Agouron Pharmaceuticals
Potent human immunodeficiency virus type 1 protease inhibitors that utilize noncoded D-amino acids as P2/P3 ligands.
Eli Lilly
Potent HIV protease inhibitors: the development of tetrahydrofuranylglycines as novel P2-ligands and pyrazine amides as P3-ligands.
Merck Research Laboratories
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors possessing augmented P2' side chains.
University of Pennsylvania
Hydroxyethylene sulfones as a new scaffold to address aspartic proteases: design, synthesis, and structural characterization.
Philipps-Universitat Marburg
The synthesis of symmetrical and unsymmetrical P1/P1' cyclic ureas as HIV protease inhibitors.
Dupont Pharmaceuticals
Preparation and structure-activity relationship of novel P1/P1'-substituted cyclic urea-based human immunodeficiency virus type-1 protease inhibitors.
Dupont Pharmaceuticals
Improved P1/P1' substituents for cyclic urea based HIV-1 protease inhibitors: synthesis, structure-activity relationship, and X-ray crystal structure analysis.
Dupont Pharmaceuticals
Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains.
Glaxosmithkline
Inhibition of wild-type and mutant human immunodeficiency virus type 1 proteases by GW0385 and other arylsulfonamides.
Glaxosmithkline
Cyclic sulfamide HIV-1 protease inhibitors, with sidechains spanning from P2/P2' to P1/P1'.
Uppsala University
Structure-activity relationship of HIV-1 protease inhibitors containing AHPBA. Part III: Modification of P2 site.
Sankyo
Structure-activity relationships of HIV-1 PR inhibitors containing AHPBA--II. Modification of pyrrolidine ring at P1' proline.
Sankyo
Structure-activity relationship of HIV-1 protease inhibitors containing alpha-hydroxy-beta-amino acids. Detailed study of P1 site.
Sankyo
Protein structure-based design of potent orally bioavailable, nonpeptide inhibitors of human immunodeficiency virus protease.
Agouron Pharmaceuticals
Structure-based design and synthesis of substituted 2-butanols as nonpeptidic inhibitors of HIV protease: secondary amide series.
Agouron Pharmaceuticals
Discovery and optimization of nonpeptide HIV-1 protease inhibitors.
Parke-Davis Pharmaceutical Research
Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety.
Parke-Davis Pharmaceutical Research
Synthesis of 5,6-dihydro-4-hydroxy-2-pyrones as HIV-1 protease inhibitors: the profound effect of polarity on antiviral activity.
Parke-Davis Pharmaceutical Research
Nonpeptidic potent HIV-1 protease inhibitors: (4-hydroxy-6-phenyl-2-oxo-2H- pyran-3-yl)thiomethanes that span P1-P2' subsites in a unique mode of active site binding.
Parke-Davis Pharmaceutical Research
Nonpeptidic HIV protease inhibitors possessing excellent antiviral activities and therapeutic indices. PD 178390: a lead HIV protease inhibitor.
Parke-Davis Pharmaceutical Research
Structure-based design of novel HIV protease inhibitors: carboxamide-containing 4-hydroxycoumarins and 4-hydroxy-2-pyrones as potent nonpeptidic inhibitors.
Upjohn
4-hydroxy-5,6-dihydropyrones. 2. Potent non-peptide inhibitors of HIV protease.
Parke-Davis Pharmaceutical Research
Stereoisomers of cyclic urea HIV-1 protease inhibitors: synthesis and binding affinities.
Dupont Pharmaceuticals
Structure-based design of nonpeptidic HIV protease inhibitors: the sulfonamide-substituted cyclooctylpyramones.
Upjohn
Potent HIV protease inhibitors containing a novel (hydroxyethyl)amide isostere.
Boehringer Ingelheim (Canada)
Inhibitors of human immunodeficiency virus type 1 protease containing 2-aminobenzyl-substituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, activity, and oral bioavailability.
Sandoz Research Institute
Structure-based design of novel HIV protease inhibitors: sulfonamide-containing 4-hydroxycoumarins and 4-hydroxy-2-pyrones as potent non-peptidic inhibitors.
Upjohn
Cyclic HIV-1 protease inhibitors derived from mannitol: synthesis, inhibitory potencies, and computational predictions of binding affinities.
Uppsala University
HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.
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 novel nonpeptide HIV-1 protease inhibitor: elucidation of the binding mode and its application in the design of related analogs.
Parke-Davis Pharmaceutical Research
Inhibitors of HIV-1 proteinase containing 2-heterosubstituted 4-amino-3-hydroxy-5-phenylpentanoic acid: synthesis, enzyme inhibition, and antiviral activity.
Sandoz Forschungsinstitut Ges.M.B.H.
Aminodiol HIV protease inhibitors. 1. Design, synthesis, and preliminary SAR.
Bristol-Myers Squibb
Crystal-structure-based design and synthesis of novel C-terminal inhibitors of HIV protease.
Agouron Pharmaceuticals
Design and synthesis of peptidomimetic inhibitors of HIV-1 protease and renin. Evidence for improved transport.
University of Pennsylvania
Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design.
Merck Research Laboratories
Benzocycloalkyl amines as novel C-termini for HIV protease inhibitors.
Merck Sharp and Dohme Research Laboratories
Potent, orally bioavailable HIV-1 protease inhibitors containing noncoded D-amino acids
Eli Lilly
In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatine.
National Cancer Institute-Bethesda
Use of medium-sized cycloalkyl rings to enhance secondary binding: discovery of a new class of human immunodeficiency virus (HIV) protease inhibitors.
Upjohn
Structure-based design of HIV protease inhibitors: 4-hydroxycoumarins and 4-hydroxy-2-pyrones as non-peptidic inhibitors.
Upjohn
Structure-based design of sulfonamide-substituted non-peptidic HIV protease inhibitors.
Upjohn
L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor.
Merck Research Laboratories
Paracyclophanes: a novel class of water-soluble inhibitors of HIV proteinase.
Sandoz Research Institute
L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.
Merck Research Laboratories
2',6'-Dimethylphenoxyacetyl: a new achiral high affinity P(3)-P(2) ligand for peptidomimetic-based HIV protease inhibitors.
Boehringer Ingelheim Pharmaceuticals
Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine.
Japan Energy
Synthesis of potent C(2)-symmetric, diol-based hiv-1 protease inhibitors. Investigation of thioalkyl and thioaryl P1/P1' substituents.
Stockholm University
Aminodiol HIV protease inhibitors. Synthesis and structure-activity relationships of P1/P1' compounds: correlation between lipophilicity and cytotoxicity.
Bristol-Myers Squibb
Synthesis and structure-activity relationships of a series of penicillin-derived HIV proteinase inhibitors containing a stereochemically unique peptide isostere.
Glaxo Group Research
A series of penicillin derived C2-symmetric inhibitors of HIV-1 proteinase: synthesis, mode of interaction, and structure-activity relationships.
Glaxo Group Research
Synthesis of novel, potent, diol-based HIV-1 protease inhibitors via intermolecular pinacol homocoupling of (2S)-2-benzyloxymethyl-4-phenylbutanal.
Stockholm University
Nonpeptidal P2 ligands for HIV protease inhibitors: structure-based design, synthesis, and biological evaluation.
University of Illinois At Chicago
Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.
Upjohn
The development of cyclic sulfolanes as novel and high-affinity P2 ligands for HIV-1 protease inhibitors.
Merck Research Laboratories
Discovery of a novel class of potent HIV-1 protease inhibitors containing the (R)-(hydroxyethyl)urea isostere.
Monsanto Corporate Research
3-Tetrahydrofuran and pyran urethanes as high-affinity P2-ligands for HIV-1 protease inhibitors.
Merck Research Laboratories
Cyclic sulfolanes as novel and high affinity P2 ligands for HIV-1 protease inhibitors.
Merck Research Laboratories
Design and synthesis of potent C(2)-symmetric diol-based HIV-1 protease inhibitors: effects of fluoro substitution.
Linkoping University
Synthesis and comparative molecular field analysis (CoMFA) of symmetric and nonsymmetric cyclic sulfamide HIV-1 protease inhibitors.
Uppsala University
SYNTHESIS AND PHARMACOKINETICS OF POTENT CARBAMATE HIV-1 PROTEASE INHIBITORS CONTAINING NOVEL HIGH AFFINITY HYDROXYETHYLAMINE ISOSTERES
Eli Lilly
Cycloalkylpiperazines as HIV-1 Protease Inhibitors: Enhanced Oral Absorption
Merck Research Laboratories
Aza-peptide analogs as potent human immunodeficiency virus type-1 protease inhibitors with oral bioavailability.
Ciba-Geigy
INFLUENCE OF STEREOCHEMISTRY ON ACTIVITY AND BINDING MODES FOR C(2) SYMMETRY-BASED DIOL INHIBITORS OF HIV-1 PROTEASE.
Nci-Fcrdc
Design, activity, and 2.8 A crystal structure of a C2 symmetric inhibitor complexed to HIV-1 protease.
Abbott Laboratories