Characterization of 3,3-dimethyl substituted N-aryl piperidines as potent microsomal prostaglandin E synthase-1 inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 26, Issue 19, 2016, Pages 4824-4828

  Kuklish, Steven L ^a   Antonysamy, Stephen ^a   Bhattachar, Shobha N ^a   Chandrasekhar, Srinivasan ^a   Fisher, Matthew J ^a   Fretland, Adrian J ^a   Gooding, Karen ^a   Harvey, Anita ^a   Hughes, Norman E ^a   Luz, John G ^a   Manninen, Peter R ^a   McGee, James E ^a   Navarro, Antonio ^a   Norman, Bryan H ^a   Partridge, Katherine M ^a   Quimby, Steven J ^a   Schiffler, Matthew A ^a   Sloan, Ashley V ^a   Warshawsky, Alan M ^a   York, Jeremy S ^a   Yu, Xiao Peng ^a   more..

^a ELI LILLY AND COMPANY   (United States)

Author keywords

Biomarker; Dog bioavailability; mPGES 1; Prostaglandin pathway

Indexed keywords

CYCLOOXYGENASE 1; CYCLOOXYGENASE 2; CYTOCHROME P450 2C9; CYTOCHROME P450 3A4; ISOMERASE INHIBITOR; MICROSOMAL PROSTAGLANDIN E SYNTHASE 1 INHIBITOR; PIPERIDINE DERIVATIVE; PROSTAGLANDIN E SYNTHASE 1; UNCLASSIFIED DRUG; PROSTAGLANDIN E SYNTHASE;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CHIRALITY; CONTROLLED STUDY; CRYSTAL STRUCTURE; DIELS ALDER REACTION; DOG; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG POTENCY; ENZYME ASSAY; EX VIVO STUDY; HUMAN; HUMAN CELL; IC50; LIVER MICROSOME METABOLISM; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PROSTAGLANDIN SYNTHESIS INHIBITION; RAT; SPECIES DIFFERENCE; STRUCTURE ACTIVITY RELATION; TIME-DEPENDENT INHIBITION; VOLUME OF DISTRIBUTION; A-549 CELL LINE; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; X RAY CRYSTALLOGRAPHY;

A549 CELLS; ANIMALS; CRYSTALLOGRAPHY, X-RAY; DOGS; HUMANS; PIPERIDINES; PROSTAGLANDIN-E SYNTHASES; RATS; SPECIES SPECIFICITY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84985917000     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2016.08.023     Document Type: Article

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