Design, synthesis and in vitro activity of glycinamide-bearing compounds as DPP-IV inhibitors.
- Author:
Bei HAN
1
;
Yi HUAN
;
Zi-Yun LIN
;
Peng LI
;
Zhu-Fang SHEN
;
Da-Li YIN
;
Hai-Hong HUANG
Author Information
1. Institute of Materia Medica, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100050, China.
- Publication Type:Journal Article
- MeSH:
Dipeptidyl Peptidase 4;
metabolism;
Dipeptidyl-Peptidase IV Inhibitors;
chemical synthesis;
chemistry;
pharmacology;
Drug Design;
Glycine;
analogs & derivatives;
chemistry;
Magnetic Resonance Spectroscopy;
methods;
Molecular Structure;
Piperazines;
chemistry;
pharmacology;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2010;45(11):1379-1384
- 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.
