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

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12 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)1274-1279
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number5
Publication statusPublished - 2007 Mar 1

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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