4-Anilinoquinoline triazines: A novel class of hybrid antimalarial agents

被引：68
|
作者：
Kumar, Ashok [1 ]
Srivastava, Kumkum [2 ]
Kumar, S. Raja [2 ]
Siddiqi, M. I. [3 ]
Puri, Sunil K. [2 ]
Sexana, Jitendra K. [4 ]
Chauhan, Prem M. S. [1 ]
机构：
[1] Cent Drug Res Inst, Div Med & Proc Chem, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst, Div Parasitol, Lucknow 226001, Uttar Pradesh, India
[3] Cent Drug Res Inst, Mol & Struct Biol Div, Lucknow 226001, Uttar Pradesh, India
[4] Cent Drug Res Inst, Div Biochem, Lucknow 226001, Uttar Pradesh, India
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 02期
关键词：
4-anilinoquinoline triazine; Antimalarial; P; falciparum; yoelii; AMODIAQUINE-INDUCED AGRANULOCYTOSIS; BETA-HEMATIN FORMATION; DIHYDROFOLATE-REDUCTASE; DRUG RESISTANCE; CHLOROQUINE RESISTANCE; POINT MUTATIONS; IN-VITRO; 2,4,6-TRISUBSTITUTED TRIAZINES; COMBINATION THERAPY; MALARIA;
D O I：
10.1016/j.ejmech.2010.12.003
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel class of hybrid 4-anilinoquinoline triazines have been synthesized and evaluated in vitro for their antimalarial activity against CQ-sensitive 3D7 strain of P. falciparum as well as for their cytotoxicity toward VERO cell line. Five compounds (19, 20, 23, 41 and 45) exhibited the antimalarial potency superior to CQ. Compounds 14 and 16 were found to be orally active at a dose of 100 mg/kg x 4 days against CQ-resistant strain of P. yoelii. Inhibition of (beta-hematin formation assay and molecular docking study has been conducted in order to gain insight into the mechanism of action of proposed targets for the 4-anilinoquinoline and triazine moiety of the hybrid compounds. (C) 2010 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：676 / 690
页数：15
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