title: Synthesis and biological evaluation of orally active hypolipidemic agents.
abstract: A series of novel fenofibric acid ester prodrugs 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.
authors.affiliation: Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur-413 255, India. bandgar_bp@yahoo.com
authors.forename: Babasaheb P
authors.initials: BP
authors.lastname: Bandgar
authors.forename: Rajendra J
authors.initials: RJ
authors.lastname: Sarangdhar
authors.forename: Fruthous
authors.initials: F
authors.lastname: Khan
authors.forename: Jeyamurugan
authors.initials: J
authors.lastname: Mookkan
authors.forename: Pranesha
authors.initials: P
authors.lastname: Shetty
authors.forename: Gajendra
authors.initials: G
authors.lastname: Singh
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002784:Cholesterol / Q000097:blood; D004952:Esters; D011345:Fenofibrate / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry; D000960:Hypolipidemic Agents / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000737:chemistry; D008297:Male; D051379:Mice; D008956:Models, Chemical; D015394:Molecular Structure; D010316:Particle Size; D011355:Prodrugs / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000737:chemistry; D014280:Triglycerides / Q000097:blood; D014961:X-Ray Diffraction
chemical_list: D004952:Esters; D000960:Hypolipidemic Agents; D011355:Prodrugs; D014280:Triglycerides; D002784:Cholesterol; C006012:fenofibric acid; D011345:Fenofibrate