Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors |
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| Authors: | Tsai Ting-Yueh Coumar Mohane Selvaraj Hsu Tsu Hsieh Hsing-Pang Chien Chia-Hui Chen Chiung-Tong Chang Chung-Nien Lo Yu-Kang Wu Ssu-Hui Huang Chung-Yu Huang Yu-Wen Wang Min-Hsien Wu Hsin-Yi Lee Hong-Jen Chen Xin Chao Yu-Sheng Jiaang Weir-Torn |
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| Institution: | Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, ROC. |
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| Abstract: | A series of substituted pyrrolidine-2,4-dicarboxylic acid amides were synthesized as potential antidiabetic agents, and many of them showed good in vitro DPP-IV inhibition (IC50 = 2-250 nM) with selectivity over DPP-II, DPP8, and FAP enzymes. Selected compounds 8c and 11a showed in vivo plasma DPP-IV inhibition after oral administration in Wistar rats. |
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