Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4′-piperidine] based melanocortin subtype-4 receptor agonists

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• 作者：Liangqin Guo ; Zhixiong Ye ; Jian Liu ; Shuwen He ; Raman K. Bakshi ; Iyassu K. Sebhat ; Peter H. Dobbelaar ; Qingmei Hong ; Tianying Jian ; James P. Dellureficio ; Nancy N. Tsou ; Richard G. Ball ; David H. Wein
• 关键词：Melanocortin subtype-4 receptor ; MC4R agonists ; Obesity ; Oral bioavailability ; Food intake ; Spiro isobenzofuran
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：15 August 2010
• 年：2010
• 卷：20
• 期：16
• 页码：4895-4900
• 全文大小：1080 K

文摘

Design, synthesis, and SAR of a series of 3H-spiro[isobenzofuran-1,4′-piperidine] based compounds as potent, selective and orally bioavailable melanocortin subtype-4 receptor (MC4R) agonists are disclosed.