Hybrid benzofuran-bisindole derivatives: New prototypes with promising anti-hyperlipidemic activities

被引：49

作者：

Sashidhara, Koneni V. ^{[1
]}

Modukuri, Ram K. ^{[1
]}

Sonkar, Ravi ^{[2
]}

Rao, K. Bhaskara ^{[1
]}

Bhatia, Gitika ^{[2
]}

机构：

[1] CSIR Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India

[2] CSIR Cent Drug Res Inst, Div Biochem, Lucknow 226001, Uttar Pradesh, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 68卷

关键词：

Benzofuran-bisindole; Lipid lowering activity; Lipoprotein metabolism; LCAT activity; Triton model; ANTIHYPERLIPIDEMIC ACTIVITY; CHOLESTEROL; DISCOVERY;

D O I：

10.1016/j.ejmech.2013.07.009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of different benzofuran bisindole hybrids were synthesized and evaluated in vitro for their antioxidant and in vivo for antidyslipidemic activity in triton WR-1339 induced hyperlipidemic rats. Among the series, compounds 4a, 4c, 4h and 4j showed significant decrease in plasma levels of total cholesterol (TC), phospholipids (PL) and triglycerides (TG) followed by increase in post heparin lipolytic activity (PHLA). In addition, the active hybrids possessed moderate antioxidant properties and increased the plasma lecithin cholesterol acyltransferase (LCAT) activity, which plays a key role in lipoprotein metabolism contributing to an increased level of HDL-C in serum. These results indicate that these hybrids constitute novel prototypes for the management of dyslipidemia. (C) 2013 Elsevier Masson SAS. All rights reserved.

引用

页码：38 / 46

页数：9

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