Synthesis of novel 3-carboxamide-benzocoumarin derivatives as orally active antithrombotic agents

被引：37

作者：

Sashidhara, Koneni V. ^{[1
]}

Kumar, Abdhesh ^{[1
]}

Kumar, Manoj ^{[1
]}

Singh, S. ^{[2
]}

Jain, Manish ^{[2
]}

Dikshit, Madhu ^{[2
]}

机构：

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

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 23期

关键词：

Synthesis; 3-Carboxamide-benzocoumarins; Antithrombotic activity; Bleeding time; Aspirin; Warfarin; INHIBITORS; PLATELETS; MECHANISM; POTENT; ASSAY;

D O I：

10.1016/j.bmcl.2011.09.100

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In an effort to develop potent antithrombotic agents, a series of novel 3-carboxamide-benzocoumarin derivatives were synthesized and screened for their in vivo antithrombotic activity. Among 20 compounds tested, the compound 12b showed the most promising antithrombotic activity which was comparable with clinically used aspirin or warfarin, but, at variance with these standard drugs, 12b did not exhibit the increased bleeding time, suggesting its potential as a novel antithrombotic agent. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：7034 / 7040

页数：7

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