Synthesis and structure-activity relationship of 2-adamantylmethyl tetrazoles as potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 2, 2014, Pages 654-660

  Ye, Xiang Yang ^a   Yoon, David ^a   Chen, Stephanie Y ^a   Nayeem, Akbar ^a   Golla, Rajasree ^a   Seethala, Ramakrishna ^a   Wang, Mengmeng ^a   Harper, Timothy ^a   Sleczka, Bogdan G ^a   Apedo, Atsu ^a   Li, Yi Xin ^a   He, Bin ^a   Kirby, Mark ^a   Gordon, David A ^a   Robl, Jeffrey A ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

11 Hydroxysteroid dehydrogenase type 1 (11 HSD1); Enzyme inhibitor; Structure activity relationships (SAR)

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE 1; ADAMANTANE DERIVATIVE; TETRAZOLE DERIVATIVE; 11BETA HYDROXYSTEROID DEHYDROGENASE; 2 ADAMANTYLMETHYL TETRAZOLE DERIVATIVE; ADAMANTANE; CARBON; CYTOCHROME P450; OXIDOREDUCTASE INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; CRYSTAL STRUCTURE; DRUG BINDING SITE; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; IC 50; MICROSOME; MOLECULAR DOCKING; NONHUMAN; PHARMACOPHORE; STRUCTURE ACTIVITY RELATION; ANIMAL EXPERIMENT; BIOLOGICAL ACTIVITY; COMPARATIVE STUDY; CONTROLLED STUDY; DRUG IDENTIFICATION; DRUG STABILITY; ENZYME ACTIVITY; HYDROGEN BOND; IC50; PROCESS OPTIMIZATION;

11Β-HYDROXYSTEROID DEHYDROGENASE TYPE 1 (11Β-HSD1); ENZYME INHIBITOR; STRUCTURE-ACTIVITY RELATIONSHIPS (SAR);

11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1; ADAMANTANE; ANIMALS; CRYSTALLOGRAPHY, X-RAY; ENZYME INHIBITORS; HUMANS; MICE; MICE, TRANSGENIC; MICROSOMES, LIVER; PROTEIN STRUCTURE, SECONDARY; STRUCTURE-ACTIVITY RELATIONSHIP; TETRAZOLES;

EID: 84891840534     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.11.066     Document Type: Article

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