| Literature DB >> 21106276 |
Jifeng Deng1, Li Peng, Guicheng Zhang, Xiaobing Lan, Chufang Li, Fuxin Chen, Yayao Zhou, Zuoxian Lin, Ling Chen, Renke Dai, Hongjiang Xu, Ling Yang, Xiquan Zhang, Wenhui Hu.
Abstract
New dipeptidyl peptidase IV inhibitors were designed based on Alogliptin using a scaffold-hopping strategy. All of the compounds constructed on a thienopyrimidine scaffold demonstrated good inhibition and selectivity for DPP-IV. Compound 10d exhibited subnanomolar (IC(50)=0.33nM) DPP-IV inhibitory activity, good in vivo efficacy and an acceptable pharmacokinetic profile. A pharmacokinetic-driven optimization of 10d may lead to a new class of clinical candidate DPP-IV inhibitors.Entities:
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Year: 2010 PMID： 21106276 DOI： 10.1016/j.ejmech.2010.10.016
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514