Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors

Journal of Medicinal Chemistry

Volumn 60, Issue 9, 2017, Pages 3594-3605

  Cernak, Tim ^a   Gesmundo, Nathan J ^a   Dykstra, Kevin ^a   Yu, Yang ^a   Wu, Zhicai ^a   Shi, Zhi Cai ^a   Vachal, Petr ^a   Sperbeck, Donald ^a   He, Shuwen ^a   Murphy, Beth Ann ^a   Sonatore, Lisa ^a   Williams, Steven ^a   Madeira, Maria ^a   Verras, Andreas ^a   Reiter, Maud ^a   Lee, Claire Heechoon ^a   Cuff, James ^a   Sherer, Edward C ^a   Kuethe, Jeffrey ^a   Goble, Stephen ^a   Perrotto, Nicholas ^a   Pinto, Shirly ^a   Shen, Dong Ming ^a   Nargund, Ravi ^a   Balkovec, James ^a   DeVita, Robert J ^a   Dreher, Spencer D ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1' [5 (5 CHLORO 1H BENZO[D]IMIDAZOL 2 YL)PYRIDIN 2 YL] 1H SPIRO [FURO[3,4 C]PYRIDINE 3,4' C]PYRIDINE 3,4' PIPERIDIN] 1 ONE; 1' [5 (5 CHLORO 1H BENZO[D]IMIDAZOL 2 YL)PYRIDIN 2 YL] 3H SPIRO 1' PIPERIDIN] 3 ONE; 1' [5 (5 CHLORO 1H BENZO[D]IMIDAZOL 2 YL)PYRIDIN 2 YL] 3H SPIRO [ISOBENZOFURAN 1,4' PIPERIDINE]; 1' [5 (5 CHLORO 1H BENZO[D]IMIDAZOL 2 YL)PYRIDIN 2 YL] 5H SPIRO [FURO[3,4 B]PYRIDINE 7,4' PIPERIDIN] 5 ONE; 2 (6 FLUOROPYRIDIN 3 YL) 5 (TRIFLUOROMETHYL) 1H BENZIMIDAZOLE; 2 [3 [5 [5 (TRIFLUOROMETHYL) 1H BENZO[D]IMIDAZOL 2 YL]PYRIDIN 2 YL] 3 AZASPIRO[5.5]UNDECAN 9 YL]ACETIC ACID; 2 [8 [5 [5 (TRIFLUOROMETHYL) 1H BENZO[D]IMIDAZOL 2 YL]PYRIDIN 2 YL] 1 OXA 8 AZASPIRO[4,5]DECAN 2 YL]ACETIC ACID; 2 [8 [5 [5 (TRIFLUOROMETHYL) 1H BENZO[D]IMIDAZOL 2 YL]PYRIDIN 2 YL] 1 OXA 8 AZASPIRO[4,5]DECAN 3 YL]ACETIC ACID; 2 [9 [5 [5 (TRIFLUOROMETHYL) 1H BENZO[D]IMIDAZOL 2 YL]PYRIDIN 2 YL] 1 OXA 9 AZASPIRO[5.5]UNDECAN 3 YL]ACETIC ACID; 2 [9 [5 [5 (TRIFLUOROMETHYL) 1H BENZO[D]IMIDAZOL 2 YL]PYRIDIN 2 YL] 1 OXA 9 AZASPIRO[5.5]UNDECAN 4 YL]ACETIC ACID; 2 [9 [5 [5 (TRIFLUOROMETHYL) 1H BENZO[D]IMIDAZOL 2 YL]PYRIDIN 2 YL] 2 OXA 9 AZASPIRO[5.5]UNDECAN 3 YL]ACETIC ACID; 2 [9 [5 [5 (TRIFLUOROMETHYL) 1H BENZO[D]IMIDAZOL 2 YL]PYRIDIN 2 YL] 3,9 DIAZASPIRO[5.5]UNDECAN 3 YL]ACETIC ACID; 3 OXO 1' [5 [5 (TRIFLUOROMETHYL) 1H BENZO[D]IMIDAZOL 2 YL]PYRIDIN 2 YL] 3H SPIRO[ISOBENZOFURAN 1,4' PIPERIDINE] 5 CARBOXYLIC ACID; 5 CHLORO 2 (6 CHLOROPYRIDIN 3 YL) 1H BENZIMIDAZOLE; 5 CHLORO 2 [6 ( 5 PHENYL 2,5 DIAZABICYCLO[2.2.1]HEPTAN 2 YL)PYRIDIN 3 YL] 1H BENZO[D]IMIDAZOLE; 9 [5 [5 (TRIFLUOROMETHYL) 1H BENZO[D]IMIDAZOL 2 YL]PYRIDIN 2 YL] 1 OXA 9 AZASPIRO[5.5]UNDECANE 3 CARBOXYLIC ACID; ACYLTRANSFERASE INHIBITOR; ANTIMETABOLITE; BENZIMIDAZOLE DERIVATIVE; DIACYLGLYCEROL ACYLTRANSFERASE 1 INHIBITOR; METHYL 4 [2 OXO 8 [5 [5 (TRIFLUOROMETHYL) 1H BENZO[D]IMIDAZOL 2 YL]PYRIDIN 2YL] 1 OXA 3,8 DIAZASPIRO[4.5]DECAN 3 YL]BENZOATE; TRIACYLGLYCEROL; UNCLASSIFIED DRUG; DIACYLGLYCEROL ACYLTRANSFERASE; ENZYME INHIBITOR;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG SYNTHESIS; ENANTIOMER; EXPERIMENTATION; FAT TOLERANCE TEST; HIGH THROUGHPUT SCREENING; IC50; IN VITRO STUDY; IN VIVO STUDY; INTRINSIC CLEARANCE; METABOLIC STABILITY; MINIATURIZATION; MOUSE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; TRIACYLGLYCEROL BLOOD LEVEL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; LIQUID CHROMATOGRAPHY; MASS SPECTROMETRY; PROTON NUCLEAR MAGNETIC RESONANCE;

CHROMATOGRAPHY, LIQUID; DIACYLGLYCEROL O-ACYLTRANSFERASE; ENZYME INHIBITORS; MASS SPECTROMETRY; PROTON MAGNETIC RESONANCE SPECTROSCOPY;

EID: 85018906961     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.6b01543     Document Type: Article

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