Paper Report for: Peters_2004_Bioorg.Med.Chem.Lett_14_1491 Reference
Title: Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents
Peters JU , Weber S , Kritter S , Weiss P , Wallier A , Boehringer M , Hennig M , Kuhn B , Loeffler BM
Ref: Bioorganic & Medicinal Chemistry Lett,
14 :1491, 2004 :
PubMed Abstract PubMedSearch: Peters 2004 Bioorg.Med.Chem.Lett 14 1491 PubMedID: 15006388 Gene_locus related to this paper: human-DPP4 Inhibitor(s) related to this paper: 5AP 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.
        
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Citations formats
Peters JU, Weber S, Kritter S, Weiss P, Wallier A, Boehringer M, Hennig M, Kuhn B, Loeffler BM (2004) Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituentsBioorganic & Medicinal Chemistry Lett 14 : 1491-3 Peters JU, Weber S, Kritter S, Weiss P, Wallier A, Boehringer M, Hennig M, Kuhn B, Loeffler BM (2004) Bioorganic & Medicinal Chemistry Lett 14 : 1491-3