Discovery and synthesis of novel substituted benzocoumarins as orally active lipid modulating agents

被引：60

作者：

Sashidhara, Koneni V. ^{[1
]}

Kumar, Manoj ^{[1
]}

Modukuri, Ram K. ^{[1
]}

Srivastava, Anuj ^{[2
]}

Puri, Anju ^{[2
]}

机构：

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

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 22期

关键词：

Synthesis; Benzocoumarin; Statins; Antidyslipidemic; LOW-DENSITY-LIPOPROTEIN; DERIVATIVES;

D O I：

10.1016/j.bmcl.2011.09.053

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of a series of benzocoumarin keto-enamine schiff bases is reported. The novel compounds were evaluated for their antihyperlipidemic activity in the hyperlipidemic hamster model. The compound 11 at a dose of 10 mg/kg body weight significantly lowered the plasma triglyceride levels (TG) by 70%, total cholesterol (TC) by 47%, accompanied by an increase in HDL-C/TC ratio by 80% in hyperlipidemic hamsters to a greater degree than the reference drugs atorvastatin and lovastatin. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：6709 / 6713

页数：5

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