Salicylic acid derivatives as simplified and novel GK small molecule activators.
- Author:
Lian-Chao HUO
1
;
Yu-Liang ZHANG
;
Lei LEI
;
Shuai-Nan LIU
;
Zhu-Fang SHEN
;
Yu-Ling WANG
;
Hong-Rui SONG
;
Zhi-Qiang FENG
Author Information
1. Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
- Publication Type:Journal Article
- MeSH:
Drug Design;
Enzyme Activation;
drug effects;
Enzyme Activators;
chemical synthesis;
chemistry;
pharmacology;
Glucokinase;
metabolism;
Hypoglycemic Agents;
chemical synthesis;
chemistry;
pharmacology;
Molecular Structure;
Salicylates;
chemical synthesis;
chemistry;
pharmacology;
Thiazoles;
pharmacology
- From:
Acta Pharmaceutica Sinica
2013;48(4):514-520
- CountryChina
- Language:Chinese
-
Abstract:
Glucokinase (GK) is a new target for the treatment of type II diabetes mellitus (T2DM). In order to find a structure-simplified small molecule GK activator, 19 salicylic acid derivatives were designed and synthesized based on new lead compound (1). Experimental results showed that the potency of compound 8h is superior to control RO-28-0450 in GK activation.