期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 55, 期 12, 页码 5951-5964出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm300592r
关键词
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Inhibition of 11 beta-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 11 beta-HSD1 in human adipocytes and exhibits good druglike properties and as a consequence was selected for clinical development.
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