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

被引：12

作者：

Bandgar, Babasaheb P. ^{[1
]}

Sarangdhar, Rajendra J. ^{[1
]}

Fruthous, Khan ^{[1
]}

Mookkan, Jeyamurugan ^{[1
]}

Chaudhary, Shilpee ^{[1
]}

Chavan, Hemant V. ^{[1
]}

Bandgar, Sunil B. ^{[2
]}

Kshirsagar, Vinayak Y. ^{[2
]}

机构：

[1] Solapur Univ, Sch Chem Sci, Med Chem Res Lab, Solapur 413255, Maharashtra, India

[2] Krishna Inst Med Sci, Karad 415110, Maharashtra, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 57卷

关键词：

Benzafibrate; Prodrugs; Hypolipidemic activity; Physicochemical properties; ALPHA-ASARONE; ANALOGS;

D O I：

10.1016/j.ejmech.2012.08.036

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 50 mg/kg/day for 8 days. Prodrugs 2, 3, 5, 6, and 7 were found to be more lipophilic than bezafibrate (la), 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. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：217 / 224

页数：8

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