934525-62-9Relevant academic research and scientific papers
(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
Yeh, Teng-Kuang,Tsai, Ting-Yueh,Hsu, Tsu,Cheng, Jai-Hong,Chen, Xin,Song, Jen-Shin,Shy, Horng-Shing,Chiou, Mei-Chun,Chien, Chia-Hui,Tseng, Ya-Ju,Huang, Chung-Yu,Yeh, Kai-Chia,Huang, Yu-Lin,Huang, Chih-Hsiang,Huang, Yu-Wen,Wang, Min-Hsien,Tang, Hung-Kuan,Chao, Yu-Sheng,Chen, Chiung-Tong,Jiaang, Weir-Torn
, p. 3596 - 3600 (2010)
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 IC50 values of 50 > 20 μM). Of these compounds, the analogues 12a, 12h and 12i exhibited a long-lasting ex vivo DPP-IV inhibition in rats.
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
Coumar, Mohane Selvaraj,Chang, Chung-Nien,Chen, Chiung-Tong,Chen, Xin,Chien, Chia-Hui,Tsai, Ting-Yueh,Cheng, Jai-Hong,Wu, Hsin-Yi,Han, Chia-Hung,Wu, Ssu-Hui,Huang, Yu-Wen,Hsu, Tsu,Hsu, Li-Jen,Chao, Yu-Sheng,Hsieh, Hsing-Pang,Jiaang, Weir-Torn
, p. 1274 - 1279 (2008/02/02)
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.
