1024036-99-4Relevant 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.
supporting information; experimental part, 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 35, (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.
