1024035-87-7Relevant academic research and scientific papers
Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: Discovery of 2-[(3 s)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]- 3-piperidyl]acetic acid (AZD4017)
Scott, James S.,Bowker, Suzanne S.,Deschoolmeester, Joanne,Gerhardt, Stefan,Hargreaves, David,Kilgour, Elaine,Lloyd, Adele,Mayers, Rachel M.,McCoull, William,Newcombe, Nicholas J.,Ogg, Derek,Packer, Martin J.,Rees, Amanda,Revill, John,Schofield, Paul,Selmi, Nidhal,Swales, John G.,Whittamore, Paul R. O.
, p. 5951 - 5964 (2012/08/07)
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.
CHEMICAL COMPOUNDS
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Page/Page column 70, (2008/12/04)
Compounds of formula (I): wherein variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are described.
