208 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
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
On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences.
University of Duisburg-Essen
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
Non-peptidyl non-covalent cathepsin C inhibitoEEr bearing a unique thiophene-substituted pyridine: Design, structure-activity relationship and anti-inflammatory activity in vivo.
Anhui Medical University
Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19.
Shionogi
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
The University of Sydney
Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors.
The University of Arizona
Structure-Based Design of a Dual-Targeted Covalent Inhibitor Against Papain-like and Main Proteases of SARS-CoV-2.
China Pharmaceutical University
Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors.
Shandong University
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.
Niddk
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
Discovery of 2-(furan-2-ylmethylene)hydrazine-1-carbothioamide derivatives as novel inhibitors of SARS-CoV-2 main protease.
Peking University
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
Peptidomimetic nitrile warheads as SARS-CoV-2 3CL protease inhibitors.
University of Alberta Edmonton
A structural screening approach to ketoamide-based inhibitors of cathepsin K.
Glaxosmithkline
New peptidomimetic rhodesain inhibitors with improved selectivity towards human cathepsins.
Johannes Gutenberg University
Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease.
Kyushu University
Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity.
Shandong University
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
Self-Masked Aldehyde Inhibitors: A Novel Strategy for Inhibiting Cysteine Proteases.
Texas A&M University
Fluorovinylsulfones and -Sulfonates as Potent Covalent Reversible Inhibitors of the Trypanosomal Cysteine Protease Rhodesain: Structure-Activity Relationship, Inhibition Mechanism, Metabolism, and In Vivo Studies.
Johannes Gutenberg University
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
N-Sulfonyl dipeptide nitriles as inhibitors of human cathepsin S: In silico design, synthesis and biochemical characterization.
University of Bonn
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
6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S.
Currently Naeja Pharmaceutical
Design and synthesis of 6-substituted amino-4-oxa-1-azabicyclo[3,2,0]heptan-7-one derivatives as cysteine proteases inhibitors.
Currently Naeja Pharmaceutical
Neuroprotective effect of synthetic chalcone derivatives as competitive dual inhibitors against ?-calpain and cathepsin B through the downregulation of tau phosphorylation and insoluble A? peptide formation.
Ewha Womans University
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
Crystal structure of Leishmania mexicana cysteine protease B in complex with a high-affinity azadipeptide nitrile inhibitor.
University of S£O Paulo
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
Design, synthesis and stepwise optimization of nitrile-based inhibitors of cathepsins B and L.
University of S£O Paulo
Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design.
Novartis Pharmaceuticals
Green asymmetric synthesis of epoxypeptidomimetics and evaluation as human cathepsin K inhibitors.
Federal University of S£O Carlos
Cytotoxicity of 4-substituted quinoline derivatives: Anticancer and antileishmanial potential.
Universidade De Mogi Das Cruzes (Umc)
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
Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors.
National Institute of Biological Sciences (Nibs)
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
Bristol-Myers Squibb
Design, synthesis and biological evaluation of inhibitors of cathepsin K on dedifferentiated chondrocytes.
Jilin University
Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity.
Texas A&M University
Enhanced tumor retention of NTSR1-targeted agents by employing a hydrophilic cysteine cathepsin inhibitor.
University of Nebraska Medical Center
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.
Smithkline Beecham Pharmaceuticals
Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis.
University of Messina
Design of Gallinamide A Analogs as Potent Inhibitors of the Cysteine Proteases Human Cathepsin L and
The University of Jordan
Can Cysteine Protease Cross-Class Inhibitors Achieve Selectivity?
University of S£O Paulo
Discovery of covalent enzyme inhibitors using virtual docking of covalent fragments.
University of Houston
Synthesis and structure-activity relationship of nitrile-based cruzain inhibitors incorporating a trifluoroethylamine-based P2 amide replacement.
Universidade De S£O Paulo
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
Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties.
Abbott Laboratories
[3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists.
Johnson and Johnson Pharmaceutical Research and Development, Beerse
RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist.
Roche Bioscience
NNC-112, NNC-687 and NNC-756, new selective and highly potent dopamine D1 receptor antagonists.
Novo Nordisk