Pyrimidine-chloroquinoline hybrids: Synthesis and antiplasmodial activity

被引：51

作者：

Chopra, Rakesh ^{[1
]}

Chibale, Kelly ^{[2
]}

Singh, Kamaljit ^{[1
]}

机构：

[1] Guru Nanak Dev Univ, UGC Ctr Adv Studies 2, Dept Chem, Amritsar 143005, Punjab, India

[2] Univ Cape Town, Inst Infect Dis & Mol Med, South African Med Res Council, Dept Chem,Drug Discovery & Dev Res Unit, ZA-7701 Rondebosch, South Africa

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2018年 / 148卷

基金：

英国医学研究理事会;

关键词：

Pyrimidine hybrids; 7-Chloroquinoline; Triazole; Huisgen 1,3-dipolar cycloaddition; Antiplasmodial studies; Lipophilicity; Binding with DNA; PLASMODIUM-FALCIPARUM MALARIA; QUINOLINE ANTIMALARIAL-DRUGS; BIOLOGICAL-ACTIVITY; RESISTANT MALARIA; IN-VITRO; HEMATIN; ARTEMISININ; DISCOVERY; AGENTS; PRIMAQUINE;

D O I：

10.1016/j.ejmech.2018.02.021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Triazole tethered 7-chloroquinoline-pyrimidine-5-carboxylate hybrids were synthesized and evaluated for antiplasmodial activity against chloroquine sensitive (CQ(s)) NF54 strain of Plasmodium falciparum. The most active hybrids of the series were further screened against the chloroquine resistant (CQ(R)) Dd2 strain of the parasite and for in vitro cytotoxicity against mammalian Vero cell lines. Further, their physicochemical properties, binding studies with hemin (monomeric & mu-oxo dimeric) and DNA [pUC-18, calf thymus (CT)] led us to plausible proposed binding mode of the most active member of the present series. (C) 2018 Elsevier Masson SAS. All rights reserved.

引用

页码：39 / 53

页数：15

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