3-[2-((2S)-2-Cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramid e analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes

Mohane Selvaraj Coumar, Chung Nien Chang, Chiung Tong Chen, Xin Chen, Chia Hui Chien, Ting Yueh Tsai, Jai Hong Cheng, Hsin Yi Wu, Chia Hung Han, Ssu Hui Wu, Yu Wen Huang, Tsu Hsu, Li Jen Hsu, Yu Sheng Chao, Hsing Pang Hsieh, Weir Torn Jiaang

研究成果: Article同行評審

12 引文 斯高帕斯(Scopus)

摘要

Based on the structures of NVP-DPP728 (1) and NVP-LAF237 (Vildagliptin, 2), three series of DPP-IV inhibitors were synthesized by linking substituted anilines, benzylamines, and phenylethylamines to (2S)-cyanopyrrolidine through a linker. More than 20 compounds were evaluated for their in vitro DPP-IV inhibition and selectivity profile over DPP-II, DPP8, and FAP enzymes. Selected compounds 5f and 7i showed in vivo plasma DPP-IV inhibition and inhibited glucose excursion in OGTT after oral administration in Wistar rats. Compound 5f (DPP-IV IC50 = 116 nM) has the potential for development as antidiabetic agent.

原文English
頁(從 - 到)1274-1279
頁數6
期刊Bioorganic and Medicinal Chemistry Letters
17
發行號5
DOIs
出版狀態Published - 2007 三月 1

All Science Journal Classification (ASJC) codes

  • 生物化學
  • 分子醫學
  • 分子生物學
  • 藥學科學
  • 藥物發現
  • 臨床生物化學
  • 有機化學

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