Design,synthesis and biological evaluation of novel drugs for metabolic syndrome / 国际药学研究杂志

ABSTRACT

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.