The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes.

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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

The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes.

Eur J Med Chem. 2011 Jan;46(1):71-6. doi: 10.1016/j.ejmech.2010.10.016. Epub 2010 Oct 26.

PubMed ID

21106276 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Alogliptin	Dipeptidyl peptidase 4	IC 50 (nM)	3.4	N/A	N/A	Details