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
收藏
页码：6709 / 6713
页数：5
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