869468-34-8Relevant academic research and scientific papers
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.
(S,S)-(+)-pseudoephedrine as chiral auxiliary in asymmetric aza-Michael reactions. Unexpected selectivity change when manipulating the structure of the auxiliary
Etxebarria, Juan,Vicario, Jose L.,Badia, Dolores,Carrillo, Luisa,Ruiz, Nerea
, p. 8790 - 8800 (2007/10/03)
The asymmetric aza-Michael reaction of metal benzylamides to α,β-unsaturated amides derived from the chiral amino alcohol (S,S)-(+)-pseudoephedrine has been studied in detail. A deep study of the most important experimental parameters (solvent, temperatur
