Synthesis and biological evaluation of ester prodrugs of benzafibrate as orally active hypolipidemic agents

A series of bezafibrate ester prodrugs 1–7 were synthesized and evaluated for hypolipidemic activity in Swiss Albino mice (SAM). Bezafibrate (1a), a hypolipidemic drug was used as a reference compound for data comparison. Among the synthesized compounds, prodrug 7 showed superior activities in decreasing triglyceride up to 30% in mice plasma after oral administration of 50mg/kg/day for 8 days. Prodrugs 2, 3, 5, 6, and 7 were found to be more lipophilic than bezafibrate (1a), indicated by partition coefficients measured in octanol-buffer system at pH 7.4. On the basis of in vivo studies, prodrug 7 emerged as new potent hypolipidemic agent. A series of bezafibrate ester prodrugs 1–7 were synthesized and evaluated for hypolipidemic activity in Swiss Albino mice (SAM) [Display omitted] ► A series of bezafibrate ester prodrugs were synthesized. ► Synthesized compounds were evaluated for in vivo hypolipidemic activity. ► Prodrug 7 emerged as new potent hypolipidemic agent.