1265593-80-3Relevant academic research and scientific papers
The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes
Deng, Jifeng,Peng, Li,Zhang, Guicheng,Lan, Xiaobing,Li, Chufang,Chen, Fuxin,Zhou, Yayao,Lin, Zuoxian,Chen, Ling,Dai, Renke,Xu, Hongjiang,Yang, Ling,Zhang, Xiquan,Hu, Wenhui
, p. 71 - 76 (2011)
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 (IC50 = 0.33 nM) 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.
