| Title : Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents - Peters_2004_Bioorg.Med.Chem.Lett_14_1491 |
| Author(s) : 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 |
|
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. |
| PubMedSearch : Peters_2004_Bioorg.Med.Chem.Lett_14_1491 |
| PubMedID: 15006388 |
| Gene_locus related to this paper: human-DPP4 |
| Inhibitor | 5AP |
| Gene_locus | human-DPP4 |
| Structure | 1RWQ |
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 substituents
Bioorganic & Medicinal Chemistry Lett
14 :1491
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