Design, synthesis and biological evaluation of novel drugs for metabolic syndrome
10.13220/j.cnki.jipr.2017.04.008
- Author:
Yun-Long SONG
1
Author Information
1. Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences
- Publication Type:Journal Article
- Keywords:
Acipimox;
Fibrates;
Metabolic syndrome;
Phenoxyalkylcarboxylic acid pharmacophore
- From:
Journal of International Pharmaceutical Research
2017;44(4):337-341
- CountryChina
- Language:Chinese
-
Abstract:
Objective To design and synthesize novel drugs for metabolic syndrome. Methods A kind of drugs treating metabolic syndrome was designed by linking acipimox with the lipid lowering function group of fibrates. Primary amine intermediates were synthesized from 4-aminophenol, 4- (aminomethyl)phenol and 4- (2-aminoethyl)phenol by 3 steps, then target compounds were obtained by coupling acipimox with these primary amine intermediates, and their hypolipidaemic activity in Triton WR-1339 induced hyperlipi daemic mice was evaluated. Results and Conclusion 5 target compounds were synthesized and identified by1H NMR and ESI MS methods. It showed that all the compounds could decrease blood-lipid, and 4c exhibited anti-hyperlipidemic activities close to the positive control(bezafibrate)in in vivo hypolipidemic activity tests. The results have good value for the discovery of novel drugs for metabolic myndrome.
