Discovery of orally active butyrolactam 11β-HSD1 inhibitors

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• 作者：Vince S.C. Yeh ; Ravi Kurukulasuriya ; Steven Fung ; Katina Monzon ; William Chiou ; Jiahong Wang ; Deanne Stolarik ; Hovis Imade ; Robin Shapiro ; Victoria Knourek-Segel et al.
• 关键词：11b-HSD1 inhibitors ; Butyrolactams ; Pharmacokinetic ; Pharmacodynamic
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：1 November 2006
• 年：2006
• 卷：16
• 期：21
• 页码：5555-5560
• 全文大小：152 K

文摘

A series of metabolically stable butyrolactam 11β-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity, pharmacokinetic, and pharmacodynamic profiles.