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Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017).
James S Scott
1 ,
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
Jun 28 2012
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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.