Triazino indole-quinoline hybrid: A novel approach to antileishmanial agents

被引：34

作者：

Sharma, Rashmi ^{[1
]}

Pandey, Anand Kumar ^{[1
]}

Shivahare, Rahul ^{[2
]}

Srivastava, Khushboo ^{[2
]}

Gupta, Suman ^{[2
]}

Chauhan, Prem M. S. ^{[1
]}

机构：

[1] CSIR, Cent Drug Res Inst, Div Med & Proc Chem, Lucknow 226031, Uttar Pradesh, India

[2] CSIR, Cent Drug Res Inst, Div Parasitol, Lucknow 226031, Uttar Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 01期

关键词：

Antileishmanial; Hybrid; In vitro; Leishmania donovani; Quinoline; Triazino-indole; VISCERAL LEISHMANIASIS; BIOLOGICAL EVALUATION; ANTIMALARIAL ACTIVITY;

D O I：

10.1016/j.bmcl.2013.11.018

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 1,2,4-triazino-[5,6b] indole-3-thione covalently linked to 7-chloro-4-aminoquinoline have been synthesized and evaluated for their in vitro activity against extracellular promastigote and intracellular amastigote form of Leishmania donovani. Among all tested compounds, compounds 7a and 7b were found to be the most active with IC50 values 1.11, 0.36 mu M and selectivity index (SI) values 67, >1111, respectively, against amastigote form of L. donovani which is several folds more potent than the standard drugs, miltefosine (IC50 = 8.10 mu M, SI = 7) and sodium stibo-gluconate (IC50 = 54.60 mu M, SI >= 7). (C) 2013 Published by Elsevier Ltd.

引用

页码：298 / 301

页数：4

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