| Literature DB >> 22691057 |
James S Scott1, Suzanne S Bowker, Joanne Deschoolmeester, Stefan Gerhardt, David Hargreaves, Elaine Kilgour, Adele Lloyd, Rachel M Mayers, William McCoull, Nicholas J Newcombe, Derek Ogg, Martin J Packer, Amanda Rees, John Revill, Paul Schofield, Nidhal Selmi, John G Swales, Paul R O Whittamore.
Abstract
Inhibition of 11β-HSD1 is an attractive mechanism for the treatment of obesity and other elements of the metabolic syndrome. We report here the discovery of a nicotinic amide derived carboxylic acid class of inhibitors that has good potency, selectivity, and pharmacokinetic characteristics. Compound 11i (AZD4017) is an effective inhibitor of 11β-HSD1 in human adipocytes and exhibits good druglike properties and as a consequence was selected for clinical development.Entities:
Mesh：
Substances：
Year: 2012 PMID： 22691057 DOI： 10.1021/jm300592r
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446