Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors

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• 作者：Guohua Zhao ; ^{guohua.zhao@bms.com} ; ^{zhaog@bms.com} ; Chet Kwon ; Aiying Wang ; James G. Robertson ; Jovita Marcinkeviciene ; Rex A. Parker ; Mark S. Kirby ; Lawrence G. Hamann
• 关键词：Piperidine ; Pyrrolidine ; Dipeptidyl peptidase IV inhibitor ; Type 2 diabetes
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：15 March, 2013
• 年：2013
• 卷：23
• 期：6
• 页码：1622-1625
• 全文大小：752 K

文摘

Synthesis and structure-activity relationship of a series of substituted piperidinyl glycine 2-cyano-4,5-methano pyrroline DPP-IV inhibitors are described. Improvement of the inhibitory activity and chemical stability of this series of compounds was respectively achieved by the introduction of bulky groups at the 4-position and 1-position of the piperidinyl glycine, leading to a series of potent and stable DPP-IV inhibitors.