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

页码：163 / 168

页数：6

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