159 articles for thisTarget
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Article Title
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Prospective Evaluation of Free Energy Calculations for the Prioritization of Cathepsin L Inhibitors.
Roche Pharmaceutical Research And Early Development (Pred)
Synthesis and biological evaluation of a water-soluble phosphate prodrug salt and structural analogues of KGP94, a lead inhibitor of cathepsin L.
Baylor University
Evaluation of dipeptide nitriles as inhibitors of rhodesain, a major cysteine protease of Trypanosoma brucei.
Johannes Gutenberg University
Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain.
Universitat Jaume I
Straightforward synthesis of 2,4,6-trisubstituted 1,3,5-triazine compounds targeting cysteine cathepsins K and S.
Cnrs
Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).
Charles River Discovery Research Services
Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry.
University Of Bonn
Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L.
Baylor University
Development of N-(Functionalized benzoyl)-homocycloleucyl-glycinonitriles as Potent Cathepsin K Inhibitors.
National Institute Of Chemistry
Structure-based design and optimization of potent inhibitors of the adenoviral protease.
Novartis Institute For Biomedical Research
Structures and bioactivities of dihydrochalcones from Metrodorea stipularis.
Universidade Federal De S£O Carlos
Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm.
Eli Lilly
3-Cyano-3-aza-ß-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins.
University Of Bonn
Cathepsin C inhibitors: property optimization and identification of a clinical candidate.
Astrazeneca
Principles and applications of halogen bonding in medicinal chemistry and chemical biology.
Eberhard-Karls University
Development of new cathepsin B inhibitors: combining bioisosteric replacements and structure-based design to explore the structure-activity relationships of nitroxoline derivatives.
University Of Ljubljana
Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement.
Boehringer Ingelheim Pharmaceuticals
Structural investigation of anti-Trypanosoma cruzi 2-iminothiazolidin-4-ones allows the identification of agents with efficacy in infected mice.
Universidade Federal De Pernambuco
Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.
Astrazeneca
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.
Astrazeneca
Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F.
University Of Bonn
Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.
Astrazeneca
Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L.
TBA
Evaluation of synthetic acridones and 4-quinolinones as potent inhibitors of cathepsins L and V.
Universidade Federal De S£O Carlos
Exploring activity cliffs in medicinal chemistry.
Rheinische Friedrich-Wilhelms-Universit£T
Structural optimization of azadipeptide nitriles strongly increases association rates and allows the development of selective cathepsin inhibitors.
University Of Bonn
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.
Ewha Womans University
Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.
Merck Research Laboratories
Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.
University Of California
Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype.
University Of Pennsylvania
Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor.
University Of Pennsylvania
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Johnson & Johnson Pharmaceutical Research & Development
Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors.
University Of Messina
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Merck Frosst Centre For Therapeutic Research
Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption.
Takeda Chemical Industries
Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors.
University Of Messina
Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent.
Glaxosmithkline
1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pka.
Merck Research Laboratories
Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease.
Merck Research Laboratories
Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.
Merck Research Laboratories
Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.
Baylor University
Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.
Merck Research Laboratories
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
Merck Research Laboratories
Allicin and derivates are cysteine protease inhibitors with antiparasitic activity.
University Of WüRzburg
2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.
Merck Research Laboratories
Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.
Schering-Plough
Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.
Merck Frosst Canada
Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors.
Baylor University
Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.
University Of Messina
Solid-phase parallel synthesis and SAR of 4-amidofuran-3-one inhibitors of cathepsin S: effect of sulfonamides P3 substituents on potency and selectivity.
Medivir
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2.
Novartis Institutes For Biomedical Research
Effect of cathepsin K inhibitors on bone resorption.
Novartis Institutes For Biomedical Research
Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides.
University Of Leipzig
4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors.
Novartis Institutes For Biomedical Research
Discovery of selective and nonpeptidic cathepsin S inhibitors.
Novartis Institutes For Biomedical Research
Effect of novel N-cyano-tetrahydro-pyridazine compounds, a class of cathepsin K inhibitors, on the bone resorptive activity of mature osteoclasts.
Korea Research Institute Of Chemical Technology
Primary amides as selective inhibitors of cathepsin K.
Merck Frosst Centre For Therapeutic Research
Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.
The Genomics Institute Of The Novartis Research Foundation
Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.
Celera Genomics
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
Celera Genomics
Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
Glaxosmithkline
Screening of electrophilic compounds yields an aziridinyl peptide as new active-site directed SARS-CoV main protease inhibitor.
University Of WüRzburg
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
Merck Frosst Centre For Therapeutic Research
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.
Glaxosmithkline
A structural screening approach to ketoamide-based inhibitors of cathepsin K.
Glaxosmithkline
Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K.
Novartis Institutes For Biomedical Research
Inhibition of lysosomal cysteine proteases by chrysotherapeutic compounds: a possible mechanism for the antiarthritic activity of Au(I).
University Of Southern California
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.
Eli Lilly
Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions.
Glaxosmithkline
Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors.
Merck Frosst Centre For Therapeutic Research
P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors.
Eli Lilly
(4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors.
Amgen
N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.
Novartis Institute Of Biomedical Research
3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity.
Ligand Pharmaceuticals
Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K-investigating P1' substituents.
Novartis Pharma
3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.
Currently Naeja Pharmaceutical
Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides.
National Research Council Of Canada
General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain.
University Of California
Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors.
Celera
Discovery of phenyl alanine derived ketoamides carrying benzoyl residues as novel calpain inhibitors.
Abbott
Design and synthesis of dual inhibitors for matrix metalloproteinase and cathepsin.
Organon K.K.
Identification of potent and selective mechanism-based inhibitors of the cysteine protease cruzain using solid-phase parallel synthesis.
University Of California
Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design.
Novartis Pharmaceuticals
Potent reversible inhibitors of the protein tyrosine phosphatase CD45.
Astrazeneca Pharmaceuticals
Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.
Merck Frosst Centre For Therapeutic Research
Development of peptidyl alpha-keto-beta-aldehydes as new inhibitors of cathepsin L--comparisons of potency and selectivity profiles with cathepsin B.
Queen'S University Belfast
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.
Smithkline Beecham Pharmaceuticals
The marine cyanobacterial metabolite gallinamide A is a potent and selective inhibitor of human cathepsin L.
University Of California
Chalcones, inhibitors for topoisomerase I and cathepsin B and L, as potential anti-cancer agents.
Cha University
Identification of new peptide amides as selective cathepsin L inhibitors: the first step towards selective irreversible inhibitors?
National Institute Of Biology
Small-molecule inhibitors of cathepsin L incorporating functionalized ring-fused molecular frameworks.
Baylor University
New aziridine-based inhibitors of cathepsin L-like cysteine proteases with selectivity for the Leishmania cysteine protease LmCPB2.8.
Johannes Gutenberg-Universit£T Mainz
Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S.
Cnrs Upr 4301
Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs.
Universit£
Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates.
Universitat Jaume I
Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins.
Irbm Science Park
Cathepsin B inhibitors: Further exploration of the nitroxoline core.
University Of Ljubljana
Optimization of dipeptidic inhibitors of cathepsin L for improved Toxoplasma gondii selectivity and CNS permeability.
University Of Michigan
2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.
Eth Zurich
Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and Trypanosoma brucei Inhibitors.
Eth Zurich
Asymmetric synthesis and evaluation of epoxy-?-acyloxycarboxamides as selective inhibitors of cathepsin L.
Federal University Of S£O Carlos
Development of Novel Peptide-Based Michael Acceptors Targeting Rhodesain and Falcipain-2 for the Treatment of Neglected Tropical Diseases (NTDs).
University Of Messina
Synthesis of a-oxycarbanilinophosphonates and their anticholinesterase activities: the most potent derivative is bound to the peripheral site of acetylcholinesterase.
Institute For Advanced Studies In Basic Sciences (Iasbs)
In vitro effects of some anabolic compounds on erythrocyte carbonic anhydrase I and II.
Balikesir University
NNC-112, NNC-687 and NNC-756, new selective and highly potent dopamine D1 receptor antagonists.
Novo Nordisk