期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 51, 期 13, 页码 3953-3960出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm800310g
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We report the discovery of potent benzamide inhibitors of 11 beta-hydroxysteroid dehydrogenase (11 beta-HSD1). The optimization and correlation of in vitro and in vivo metabolic stability will be described. Through modifications to our initial lead 2, we discovered pyridyl compound 13. This compound has a favorable pharmacokinetic profile across three species and showed a dose-dependent decrease in adipose 11 beta-HSD1 activity in a monkey ex vivo pharmacodynamic model.
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