RESUMEN
Objective To design and synthesize novel drugs for metabolic syndrome. Methods A kind of drugs treating met?abolic 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 ob?tained by coupling acipimox with these primary amine intermediates,and their hypolipidaemic activity in Triton WR-1339 induced hy?perlipi daemic mice was evaluated. Results and Conclusion 5 target compounds were synthesized and identified by 1H 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.
RESUMEN
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.