Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.

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Peters JU, Weber S, Kritter S, Weiss P, Wallier A, Boehringer M, Hennig M, Kuhn B, Loeffler BM

Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1491-3.

PubMed ID

15006388 [ View in PubMed

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Abstract

The influence of aromatic substitution on a newly discovered class of inhibitors of dipeptidyl peptidase IV was investigated. A 10(5)-fold increase in potency was achieved by the optimization of aromatic substituents in a parallel chemistry program. The observed SAR could be explained by an X-ray structure of the protein-ligand complex.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
5-(Aminomethyl)-6-(2,4-Dichlorophenyl)-2-(3,5-Dimethoxyphenyl)Pyrimidin-4-Amine	Dipeptidyl peptidase 4	IC 50 (nM)	0.1	7.5	22	Details