Design, Synthesis and In Vitro Antimalarial Evaluation of New Quinolinylhydrazone Derivatives

被引：0
|
作者：
Le Thi Thuy [1 ]
Hoang Xuan Tien [1 ]
Vu Dinh Hoang [1 ]
Tran Khac Vu [1 ]
机构：
[1] Hanoi Univ Sci & Technol, Dept Pharmaceut Chem & Pesticides Technol, Sch Chem Engn, Hanoi, Vietnam
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2012年 / 9卷 / 02期
关键词：
Amodiaquine; Chloroquine; Hydrazone; Malarial; Plasmodium falciparum; Quinoline; PLASMODIUM-FALCIPARUM; METAL-COMPLEXES; SCHIFF-BASES; 4-AMINOQUINOLINES; INHIBITION; GROWTH; RING;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel quinolinylhydrazones (5a-f) was synthesized by the condensation reaction of 2,6-diaryl-substituted piperidin-4-ones (4a-f) with 7-chloro-4-hydrazinoquinoline (2). Novel quinolinylhydrazones containing Shiff bases 8a-f and 11a-f were obtained via the condensation of Shiff bases 7a-f and 10a-f with 7-chloro-4-hydrazinoquinoline. These synthesized hydrazones were screened for their in vitro antimalarial activities to chloroquine - sensitive (T96) and chloroquine - resistant (K1) strains of P. falciparum. Among the synthesized compounds, 11a exhibited strong antimalarial activity at IC50 of 103.4 ng/mL and 18.76 ng/mL to both strains of P. falciparum, respectively.
引用
收藏
页码：163 / 168
页数：6
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