Synthesis and biological evaluation of a new class of 4-aminoquinoline-rhodanine hybrid as potent anti-infective agents

被引：54

作者：

Chauhan, Kuldeep ^{[1
]}

Sharma, Moni ^{[1
]}

Saxena, Juhi ^{[2
]}

Singh, Shiv Vardan ^{[3
]}

Trivedi, Priyanka ^{[4
]}

Srivastava, Kumkum ^{[2
]}

Puri, Sunil K. ^{[2
]}

Saxena, J. K. ^{[3
]}

Chaturvedi, Vinita ^{[4
]}

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

机构：

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

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

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

[4] Cent Drug Res Inst, CSIR, Drug Target Discovery & Dev Div, Lucknow 226001, Uttar Pradesh, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 62卷

关键词：

4-Aminoquinoline; Rhodanine; Antimalarial; Antitubercular; Cytotoxicity; IN-VITRO; ANTIPLASMODIAL ACTIVITY; ANTIMALARIAL AGENTS; SIDE-CHAIN; RHODANINE; MALARIA; DISCOVERY; DESIGN; ASSAY; BURDEN;

D O I：

10.1016/j.ejmech.2013.01.017

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis of novel 4-aminoquinoline-rhodanine hybrid using inexpensive starting materials via easy to operate methodology, and their biological activity is reported. All the compounds were screened for their in vitro antimalarial activity against chloroquine-resistant (1(1) and chloroquine-sensitive (3D7) strains of Plasmodium falciparum, and their cytotoxicity toward VERO cell line. Compounds 9, 19, 21 and 23 exhibited excellent antimalarial activity with IC50 value ranging from 13.2 to 45.5 nM against chloroquine-resistant (K1) strain. Biochemical studies revealed that inhibition of hemozoin formation is the primary mechanism of action of these analogs for their antimalarial activity. Additionally, some derivatives (14, 18 and 26) of this series also exhibited the antimycobacterial activity against H(37)Rv strain of Mycobacterium tuberculosis with MIC value of 6.25 mu M. (C) 2013 Elsevier Masson SAS. All rights reserved.

引用

页码：693 / 704

页数：12

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