Design, synthesis and in vitro activity of glycinamide-bearing compounds as DPP-IV inhibitors.
- Author:
Bei HAN
;
Yi HUAN
;
Ziyun LIN
;
Peng LI
;
Zhufang SHEN
;
Dali YIN
;
Haihong HUANG
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2010;45(11):1379-84
- CountryChina
- Language:Chinese
-
Abstract:
To research the structure-activity relationship (SAR) of glycinamide-bearing compounds that used as inhibitors of dipeptidyl peptidase IV (DPP-IV), P32/98 and compound A were chosen as the leading compounds, heterocycles containing nitrogen atom were introduced to form amide, and different residues on a-position of carbonyl were designed. The nineteen designed compounds were synthesized by a simple route and were evaluated as inhibitors of DPP-IV. All of the structures were characterized by 1H NMR and HRMS. The preliminary SAR result was obtained.