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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)

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, 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, etc.

J Med Chem. 2012 Jun 28;55(12):5951-64.

PMID: 22691057

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
LS793634	3-(cyclohexylcarbamoyl)-5-fluorobenzeneboronic acid			Price

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