Discovery of potent, selective chymase inhibitors via fragment linking strategies

Journal of Medicinal Chemistry

Volumn 56, Issue 11, 2013, Pages 4465-4481

  Taylor, Steven J ^a   Padyana, Anil K ^a   Abeywardane, Asitha ^a   Liang, Shuang ^a   Hao, Ming Hong ^c   De Lombaert, Stéphane ^d   Proudfoot, John ^a   Farmer, Bennett S ^a   Li, Xiang ^a   Collins, Brandon ^a   Martin, Leslie ^a   Albaugh, Daniel R ^a   Hill Drzewi, Melissa ^b   Pullen, Steven S ^a   Takahashi, Hidenori ^a  

^a BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

^b BRISTOL MYERS SQUIBB   (United States)

^c EISAI INC   (United States)

^d Karos Pharmaceuticals   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [3 (6 BROMO 2 OXO 2,3 DIHYDRO 1H INDOL 4 YLMETHYL) 2 OXO 2,3 DIHYDROBENZOIMIDAZOL 1 YLMETHYL]HEXANOIC ACID; 3 [2 OXO 3 (2 OXO 2,3 DIHYDRO 1 H INDOL 4 YLMETHYL) 2,3 DIHYDROBENZOIMIDAZOL 1 YL]HEXANOIC ACID; 3 [3 (5 BROMO 2 OXO 2,3 DIHYDROBENZOTHIAZOL 7 YLMETHYL) 2 OXO 2,3 DIHYDROBENZOIMIDAZOL 1 YL]HEXANOIC ACID; 3 [3 (6 BROMO 2 OXO 2,3 DIHYDRO 1H INDOL 4 YLMETHYL) 2 OXO 2,3 DIHYDROBENZOIMIDAZOL 1 YL]HEXANOIC ACID; 3 [3 (6 BROMO 2 OXO 2,3 DIHYDRO 1H INDOL 4 YLMETHYL) 2 OXO 2,3 DIHYDROBENZOIMIDAZOL 1 YL]PROPIONIC ACID; 3 [3 (6 CHLORO 2 OXO 2,3 DIHYDRO 1H INDOL 4 YLMETHYL) 2 OXO 2,3 DIHYDROBENZOIMIDAZOL 1 YL]HEXANOIC ACID; 3 [3 (6 CHLORO 2 OXO 2,3 DIHYDRO 1H INDOL 4 YLMETHYL) 2 OXO 2,3 DIHYDROBENZOIMIDAZOL 1 YL]PROPIONIC ACID; 4 [1 (6 CHLORO 2 OXO 2,3 DIHYDRO 1H INDOL 4 YLMETHYL) 1H BENZOIMIDAZOL 2 YLSULFANYL]BUTYRIC ACID; CATHEPSIN G; CHYMASE INHIBITOR; HEXANOIC ACID DERIVATIVE; OXINDOLE; UNCLASSIFIED DRUG;

ARTICLE; DRUG IDENTIFICATION; DRUG SCREENING; FRAGMENTATION REACTION; HOMEOSTASIS; PHYSICAL CHEMISTRY; PROCESS OPTIMIZATION; X RAY CRYSTALLOGRAPHY;

BENZIMIDAZOLES; CARDIOVASCULAR AGENTS; CATALYTIC DOMAIN; CHYMASES; CRYSTALLOGRAPHY, X-RAY; HUMANS; MICROSOMES, LIVER; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN BINDING; SERINE PROTEINASE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84879056254     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm400138z     Document Type: Article

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