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]
- 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