Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: Discovery of 2-[(3 s)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]- 3-piperidyl]acetic acid (AZD4017)

Journal of Medicinal Chemistry

Volumn 55, Issue 12, 2012, Pages 5951-5964

  Scott, James S ^a   Bowker, Suzanne S ^a   Deschoolmeester, Joanne ^a   Gerhardt, Stefan ^a   Hargreaves, David ^a   Kilgour, Elaine ^a   Lloyd, Adele ^a   Mayers, Rachel M ^a   McCoull, William ^a   Newcombe, Nicholas J ^a   Ogg, Derek ^a   Packer, Martin J ^a   Rees, Amanda ^a   Revill, John ^a   Schofield, Paul ^a   Selmi, Nidhal ^a   Swales, John G ^a   Whittamore, Paul R O ^a  

^a ASTRAZENECA   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

(2 PROPYLSULFANYL 3 PYRIDYL) [2(4 PYRIDYL)PYRROLIDIN 1 YL] METHANONE; 1 [5 (CYCLOHEXYLCARBAMOYL) 6 PROPYLSULFANYLPYRIDIN 2 YL PIPERIDINE 2 CARBOXYLIC ACID; 1 [5 (CYCLOHEXYLCARBAMOYL) 6 PROPYLSULFANYLPYRIDIN 2 YL] PIPERIDINE 3 CARBOXYLIC ACID; 1 [5 (CYCLOHEXYLCARBAMOYL) 6 PROPYLSULFANYLPYRIDIN 2 YL] PIPERIDINE 4 CARBOXYLIC ACID; 11BETA HYDROXYSTEROID DEHYDROGENASE 1 INHIBITOR; 2 [1 [5 (CYCLOHEXYLCARBAMOYL) 6 (METHYLPROPYLAMINO) PYRIDIN 2 YL] 3 PIPERIDYL]ACETIC ACID; 2 [1 [5 (CYCLOHEXYLCARBAMOYL) 6 PROPOXYPYRIDIN 2 YL] 3 PIPERIDYL]ACETIC ACID; 2 [1 [5 (CYCLOHEXYLCARBAMOYL) 6 PROPYLAMINOPYRIDIN 2 YL] 3 PIPERIDYL]ACETIC ACID; 2 [1 [5 (CYCLOHEXYLCARBAMOYL) 6 PROPYLSULFANYLPYRIDIN 2 YL] 3 PIPERIDYL]ACETIC ACID; 2 [1 [5 (CYCLOHEXYLCARBAMOYL) 6 PROPYLSULFANYLPYRIDIN 2 YL] 4 PIPERIDYL]ACETIC ACID; 2 [3 [5 (CYCLOHEXYLCARBAMOYL) 6 PROPYLSULFANYLPYRIDIN 2 YL]OXYPHENYL]ACETIC ACID; 2 [4 [5 (CYCLOHEXYLCARBAMOYL) 6 PROPYLSULFANYLPYRIDIN 2 YL]OXYPHENYL]ACETIC ACID; 3 CHLORO 2 METHYL N [4 [2 (4 METHYL 1 PIPERAZINYL) 2 OXOETHYL] 2 THIAZOLYL]BENZENESULFONAMIDE; 4 [(2 PROPYLSULFANYLPYRIDINE 3 CARBONYL)AMINO] CYCLOHEXANECARBOXYLIC ACID; 4 [[5 (CYCLOHEXYLCARBAMOYL) 6 PROPYLSULFANYLPYRIDIN 2 YL] AMINO]CYCLOHEXANE 1 CARBOXYLIC ACID; 4 [[[5 (CYCLOHEXYLCARBAMOYL) 6 PROPYLSULFANYLPYRIDIN 2 YL] AMINO]METHYL]CYCLOHEXANE 1 CARBOXYLIC ACID; AMG 311; AZD 4017; BVT 14225; BVT 83370; CARBENOXOLONE; CARBOXYLIC ACID DERIVATIVE; N (4,4 DIFLUOROCYCLOHEXYL) 2 PROPYLSULFANYLPYRIDINE 3 CARBOXAMIDE; N (5 HYDROXY 2 ADAMANTYL) 2 PROPYLSULFANYLPYRIDINE 3 CARBOXAMIDE; N (5 HYDROXY 2 ADAMANTYL) N METHYL 2 PROPYLSULFANYLPYRIDINE 3 CARBOXAMIDE; N CYCLOHEXYL 2 PROPYLSULFANYLPYRIDINE 3 CARBOXAMIDE; N CYCLOHEXYL N METHYL 2 PROPYLSULFANYLPYRIDINE 3 CARBOXAMIDE; N METHYL 2 PROPYLSULFANYL N TETRAHYDROPYRAN 4 YL PYRIDINE 3 CARBOXAMIDE; OXIDOREDUCTASE INHIBITOR; PF 915275; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ADIPOCYTE; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; HUMAN; HUMAN TISSUE; MALE; MOUSE; NONHUMAN;

11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1; ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; DOGS; DRUG DISCOVERY; ENZYME INHIBITORS; HUMANS; INHIBITORY CONCENTRATION 50; MALE; MICE; MODELS, MOLECULAR; NIACINAMIDE; PIPERIDINES; PROTEIN CONFORMATION; RATS; SUBSTRATE SPECIFICITY;

EID: 84863086678     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm300592r     Document Type: Article

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