2. Academic Validation
  3. (2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV

(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV

  • Bioorg Med Chem Lett. 2010 Jun 15;20(12):3596-600. doi: 10.1016/j.bmcl.2010.04.124.
Teng-Kuang Yeh 1,  Ting-Yueh Tsai,  Tsu Hsu,  Jai-Hong Cheng,  Xin Chen,  Jen-Shin Song,  Horng-Shing Shy,  Mei-Chun Chiou,  Chia-Hui Chien,  Ya-Ju Tseng,  Chung-Yu Huang,  Kai-Chia Yeh,  Yu-Lin Huang,  Chih-Hsiang Huang,  Yu-Wen Huang,  Min-Hsien Wang,  Hung-Kuan Tang,  Yu-Sheng Chao,  Chiung-Tong Chen,  Weir-Torn Jiaang
Affiliations

Affiliation

  • 1 Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Zhunan Town, Miaoli Country, Taiwan, ROC.
PMID: 20483603 DOI: 10.1016/j.bmcl.2010.04.124
Abstract

A series of 2-[3-[2-[(2S)-2-cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-based DPP-IV inhibitors with various monocyclic amines were synthesized. The structure-activity relationships (SAR) led to the discovery of potent DPP-IV inhibitors, having IC(50) values of <100 nM with excellent selectivity over the closely related enzymes, DPP-II, DPP8, DPP9 and FAP (IC(50)>20 microM). Of these compounds, the analogues 12a, 12h and 12i exhibited a long-lasting ex vivo DPP-IV inhibition in rats.

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