Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors

L Wang, B Zhang, J Ji, B Li, J Yan, W Zhang…

文献索引：Wang, Liutang; Zhang, Bin; Ji, Jianxin; Li, Bogang; Yan, Jufang; Zhang, Weiyu; Wu, Yong; Wang, Xuechao European Journal of Medicinal Chemistry, 2009 , vol. 44, # 8 p. 3318 - 3322

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被引用次数: 9

摘要

To find potent and selective inhibitors of dipeptidyl peptidase IV (DPP-IV), we synthesized a series of 2-cyanopyrrolidine derivatives with constrained imidazolidin ring and tested their activities against DPP-IV. Most of them exhibited submicromolar inhibitory activities against DPP-IV. The most potent compound among these is (S)-1-(2-(2-(3-(3, 4-dimethoxyphenyl)-2- oxoimidazolidin-1-yl) ethyl-amino) acetyl) pyrrolidine-2-carbonitrile (6n), which is a 2nM ...