Synthesis and Biological Evaluation of Orally Active Hypolipidemic Agents
摘要:
A series of novel fenofibric acid ester pro drugs 1c-1h were synthesized and evaluated with the aim of obtaining potent hypolipidemic agents. Prodrugs 1c and 1d exhibited potent hypochlolesterolemic activity, lowering the mice plasma triglyceride level up to 47% in Swiss albino mice after oral administration of 50 mg/kg/day for 8 days. Fenofibric acid ester prodrugs 1c-1h were found lipophilic like fenofibrate (1b), indicated by partition coefficients measured in octanol-buffer system at pH 7.4. On the basis of in vivo studies, prodrugs 1c and 1d emerged as potent hypolipidemic agents.
Synthesis and Biological Evaluation of Orally Active Hypolipidemic Agents
作者:Babasaheb P. Bandgar、Rajendra J. Sarangdhar、Fruthous Khan、Jeyamurugan Mookkan、Pranesha Shetty、Gajendra Singh
DOI:10.1021/jm200704f
日期:2011.8.25
A series of novel fenofibric acid ester pro drugs 1c-1h were synthesized and evaluated with the aim of obtaining potent hypolipidemic agents. Prodrugs 1c and 1d exhibited potent hypochlolesterolemic activity, lowering the mice plasma triglyceride level up to 47% in Swiss albino mice after oral administration of 50 mg/kg/day for 8 days. Fenofibric acid ester prodrugs 1c-1h were found lipophilic like fenofibrate (1b), indicated by partition coefficients measured in octanol-buffer system at pH 7.4. On the basis of in vivo studies, prodrugs 1c and 1d emerged as potent hypolipidemic agents.