2. Academic Validation
  3. 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)

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)

  • J Med Chem. 2012 Jun 28;55(12):5951-64. doi: 10.1021/jm300592r.
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
Affiliations

Affiliation

  • 1 Cardiovascular and Gastrointestinal Innovative Medicines Unit, AstraZeneca Mereside, Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK. jamie.scott@astrazeneca.com
PMID: 22691057 DOI: 10.1021/jm300592r
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.

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