The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27690432 |
75 |
Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986). |
Charles River Discovery Research Services |
25599836 |
14 |
Multi-parameter optimization of aza-follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 2: Impact of lipophilicity on promiscuity and in vivo toxicity. |
Boehringer Ingelheim (Canada) |
25650311 |
76 |
Synthesis and pharmacological characterization of 2-aminobenzaldehyde oxime analogs as dual inhibitors of neutrophil elastase and proteinase 3. |
Chang Gung University |
24524217 |
65 |
Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates. |
Hokkaido University |
24224573 |
31 |
Optimization of O3-acyl kojic acid derivatives as potent and selective human neutrophil elastase inhibitors. |
Universidade De Lisboa |
23719288 |
41 |
Discovery of novel series of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as human chymase inhibitors using structure-based drug design. |
Asubio Pharma |
23659209 |
30 |
Discovery of potent, selective chymase inhibitors via fragment linking strategies. |
Boehringer Ingelheim Pharmaceuticals |
16644215 |
52 |
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors. |
Celera Genomics |
22882079 |
26 |
Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase. |
Aarhus University |
22595175 |
18 |
N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases. |
University Of Lisbon |
18995931 |
16 |
Natural polyprenylated benzophenones inhibiting cysteine and serine proteases. |
Federal University Of Alfenas |
17535802 |
91 |
Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing. |
Merck Research Laboratories |
18247547 |
6 |
Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer. |
Cephalon |
12190311 |
37 |
Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151). |
Gsk |
11312928 |
62 |
Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic difluoromethylene ketones as novel inhibitors of human chymase. |
Welfide |
11312927 |
64 |
Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic alpha-keto heterocycles as novel inhibitors of human chymase. |
Welfide |
1578486 |
53 |
Novel anthraquinone inhibitors of human leukocyte elastase and cathepsin G. |
Georgia Institute Of Technology |
21733690 |
40 |
Benzimidazolone as potent chymase inhibitor: modulation of reactive metabolite formation in the hydrophobic (P1) region. |
Boehringer Ingelheim Pharmaceuticals |
20925433 |
21 |
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives. |
Aristotle University Of Thessaloniki |
19483697 |
23 |
Phage-encoded combinatorial chemical libraries based on bicyclic peptides. |
Laboratory Of Molecular Biology, Medical Research Council |
20102150 |
35 |
Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif. |
Johnson & Johnson Pharmaceutical Research And Development |
19665376 |
48 |
Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C. |
Merck Frosst Canada |
19908842 |
84 |
Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB. |
National Human Genome Research Institute |
| 7 |
Janus compounds: dual inhibitors of proteinases |
TBA |
19362846 |
1 |
Introduction of non-natural amino acid residues into the substrate-specific P1 position of trypsin inhibitor SFTI-1 yields potent chymotrypsin and cathepsin G inhibitors. |
University Of Gda£?Sk |
18701300 |
55 |
Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides. |
University Of Leipzig |
17434735 |
34 |
Development of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as orally active human chymase inhibitors. |
Daiichi Asubio Pharma |
17419055 |
30 |
Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors. |
Daiichi Asubio Pharma |
17361995 |
31 |
Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase. |
Johnson & Johnson Pharmaceutical Research And Development |
14761180 |
31 |
Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G. |
Johnson & Johnson Pharmaceutical Research & Development |
14592513 |
24 |
Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors. |
Toa Eiyo |
11425539 |
23 |
Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones. |
Shionogi |
11078188 |
20 |
1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma. |
Shionogi |
11078187 |
36 |
Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors. |
Shionogi |
10698435 |
150 |
Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors. |
Kyoto Pharmaceutical University |
10091694 |
90 |
Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors. |
Nippon Steel |
9925737 |
57 |
N-[2,2-dimethyl-3-(N-(4-cyanobenzoyl)amino)nonanoyl]-L-phenylalanine ethyl ester as a stable ester-type inhibitor of chymotrypsin-like serine proteases: structural requirements for potent inhibition of alpha-chymotrypsin. |
Nippon Steel |
9871680 |
5 |
Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids. |
Proscript |
9767628 |
31 |
Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition. |
Glaxowellcome Medicines Research Centre |
9379436 |
46 |
Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase. |
Zeneca Pharmaceuticals |
9341916 |
30 |
Anionic- and lipophilic-mediated surface binding inhibitors of human leukocyte elastase. |
RhôNe-Poulenc Rorer |
9216834 |
153 |
Substituted 3-(phenylsulfonyl)-1-phenylimidazolidine-2,4-dione derivatives as novel nonpeptide inhibitors of human heart chymase. |
Suntory |
7837244 |
33 |
Non-peptidic inhibitors of human leukocyte elastase. 4. Design, synthesis, and in vitro and in vivo activity of a series of beta-carbolinone-containing trifluoromethyl ketones. |
Zeneca Pharmaceuticals |
7739010 |
118 |
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin. |
Thrombosis Research Institute |
7629790 |
32 |
New orally active serine protease inhibitors. |
Minase Research Institute |
7562931 |
41 |
Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles. |
Zeneca Pharmaceuticals |
2296031 |
48 |
Synthesis of peptidyl fluoromethyl ketones and peptidyl alpha-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, and rat and human neutrophil cathepsin G. |
Merrell Dow Research Institute |
10715152 |
151 |
5,6-Dihydropyran-2-ones possessing various sulfonyl functionalities: potent nonpeptidic inhibitors of HIV protease. |
Parke-Davis Pharmaceutical Research |