Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin e Synthase-1 Inhibitors

Journal of Medicinal Chemistry

Volumn 59, Issue 1, 2016, Pages 194-205

  Schiffler, Matthew A ^a   Antonysamy, Stephen ^a   Bhattachar, Shobha N ^a   Campanale, Kristina M ^a   Chandrasekhar, Srinivasan ^a   Condon, Bradley ^a   Desai, Prashant V ^a   Fisher, Matthew J ^a   Groshong, Christopher ^a   Harvey, Anita ^a   Hickey, Michael J ^a   Hughes, Norman E ^a   Jones, Scott A ^a   Kim, Euibong J ^a,b   Kuklish, Steven L ^a   Luz, John G ^a   Norman, Bryan H ^a   Rathmell, Richard E ^a   Rizzo, John R ^a   Seng, Thomas W ^a   Thibodeaux, Stefan J ^a,c   Woods, Timothy A ^a   York, Jeremy S ^a   Yu, Xiao Peng ^a   more..

^a ELI LILLY AND COMPANY   (United States)

^b Mongolia International University   (Mongolia)

^c NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 (DIFLUOROMETHYL) 5 (ISOBUTYRAMIDOMETHYL) N [4 METHYL 5 [4 (TRIFLUOROMETHYL)PHENYL] 1H IMIDAZOL 2 YL]NICOTAMIDE PHOSPHORIC ACID SALT; 2 (DIFLUOROMETHYL) 5 (ISOBUTYRAMIDOMETHYL) N [4 METHYL 5 [4 (TRIFLUOROMETHYL)PHENYL] 1H IMIDAZOL 2 YL]NICOTINAMIDE; 2 BROMO 1 [4 (TRIFLUOROMETHYL)PHENYL] 1 PROPANONE; 2 CHLORO 5 (PIVALAMIDOMETHYL)BENZOIC ACID; 2 CHLRO N (1H IMIDAZOL 2 YL) 5 (PIVALAMIDOMETHYL) BENZAMIDE; 2 METHYL 3 [4 (TRIFLUOROMETHYL)PHENYL]IMIDAZOL[1,2 ALPHA] PYRIMIDINE; 4 METHYL 5 [4 (TRIFLUOROMETHYL)PHENYL] 1H IMIDAZO 2 AMINE; BIOLOGICAL MARKER; CELECOXIB; CYTOCHROME P450 3A4; IMIDAZOLE DERIVATIVE; ISOMERASE INHIBITOR; KETONE; PROSTAGLANDIN E SYNTHASE 1; UNCLASSIFIED DRUG; ANALGESIC AGENT; CYTOCHROME P450 3A; CYTOCHROME P450 INHIBITOR; ISOMERASE; NONSTEROID ANTIINFLAMMATORY AGENT; PROSTAGLANDIN E SYNTHASE; PROSTAGLANDIN SYNTHASE INHIBITOR;

ACYLATION; ANIMAL CELL; ANIMAL EXPERIMENT; ANTINOCICEPTION; ARTICLE; BROMINATION; CRYSTAL STRUCTURE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG EXCRETION; DRUG FORMULATION; DRUG METABOLISM; DRUG POTENCY; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION ASSAY; HUMAN; HUMAN CELL; LIPOPHILICITY; MALE; MELTING POINT; NONHUMAN; PHYSICAL CHEMISTRY; QT PROLONGATION; RAT; SAPONIFICATION; STRUCTURE ACTIVITY RELATION; THERMODYNAMICS; WETTABILITY; ANIMAL; ANTAGONISTS AND INHIBITORS; BIOAVAILABILITY; CHEMICAL STRUCTURE; DOG; DRUG DEVELOPMENT; DRUG EFFECTS; ENZYMOLOGY; MICROSOME; SYNTHESIS;

ANALGESICS; ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; BIOLOGICAL AVAILABILITY; CELECOXIB; CYCLOOXYGENASE INHIBITORS; CYTOCHROME P-450 CYP3A; CYTOCHROME P-450 ENZYME INHIBITORS; DOGS; DRUG DISCOVERY; HUMANS; IMIDAZOLES; INTRAMOLECULAR OXIDOREDUCTASES; MICROSOMES; MODELS, MOLECULAR; RATS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84955084220     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b01249     Document Type: Article

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