Design, synthesis and biological evaluation of novel drugs for metabolic syndrome / 国际药学研究杂志
Journal of International Pharmaceutical Research
;
(6): 337-341, 2017.
Article
in Chinese
| WPRIM
| ID: wpr-845380
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.
Full text:
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Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Journal of International Pharmaceutical Research
Year:
2017
Type:
Article
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