Synthesis and Antimalarial Activity of 7-Chloro-4-(4-(2-(Oxo, Hydroxyl & Fluoro-2-1 (4-Phenyl)Ethyl)Piperazin-1-yl)Quinoline Derivatives

被引:0
|
作者
Mahajan, Akhil [1 ]
Chundawat, Tejpal Singh [1 ]
机构
[1] NorthCap Univ, Dept Appl Sci, Gurugram, India
来源
BIOINTERFACE RESEARCH IN APPLIED CHEMISTRY | 2022年 / 12卷 / 06期
关键词
piperazine; quinoline; synthesis; antimalarial activity; PLASMODIUM-FALCIPARUM; QUINOLINE; ANTIBACTERIAL; PIPERAZINE; ANALOGS; DESIGN;
D O I
10.33263/BRIAC126.79577971
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
Since these days, microbes are resistant to the drugs available in the market, which has caused an alarming impact on society. 18 compounds in a series of 7-chloro-4-(piperazin-1-yl)quinoline derivatives were synthesized by nucleophilic addition reaction of piperazine with 4,7-dichloroquinoline followed by phenacyl bromides addition to heteroaryl piperazine and then reduction and fluorination. All 18 compounds were evaluated in vitro for their antimalarial activity against plasmodium falciparum strain. Although 12 compounds showed good activity, compound 3c was found to be more potent than standard drug Quinine having MIC 0.18 mu g/mL. On the other hand, 3d, 3e, 5a, and 5f were found to be equipotent (MIC 0.26 mu g/mL) to the standard drug.
引用
收藏
页码:7957 / 7971
页数:15
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