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  • Title: The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes.
    Author: Deng J, Peng L, Zhang G, Lan X, Li C, Chen F, Zhou Y, Lin Z, Chen L, Dai R, Xu H, Yang L, Zhang X, Hu W.
    Journal: Eur J Med Chem; 2011 Jan; 46(1):71-6. PubMed ID: 21106276.
    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.
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