Synthesis and antimalarial evaluation of novel pyridine quinoline hybrids

被引：57

作者：

Acharya, Badri Narayan ^{[1
]}

Thavaselvam, D. ^{[2
]}

Kaushik, Mahabir Parshad ^{[1
]}

机构：

[1] Def Res & Dev Estab, Discovery Ctr, Gwalior 474002, MP, India

[2] Def Res & Dev Estab, Div Microbiol, Gwalior 474002, MP, India

来源：

MEDICINAL CHEMISTRY RESEARCH | 2008年 / 17卷 / 08期

关键词：

malaria; P; falciparum; haem detoxification; hematin; pyridine-quinoline hybrid molecules;

D O I：

10.1007/s00044-008-9092-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis and evaluation of the antimalarial activity of new pyridine quinoline hybrid molecules against a chloroquine-susceptible strain of Plasmodium falciparum and as inhibitors of beta-hematin formation are described. Two novel pyridine quinoline hybrid molecules and one bisquinoline molecule were synthesized and purified by column chromatography and evaluated for antimalarial and haem polymerization inhibition (HPIA) activities. The molecules were found to be very good haem polymerization inhibitors but showed poor antimalarial activity. This was attributed to their low vacuole accumulation ratio (VAR) in comparison to chloroquine. These molecules can be used as templates for designing new antimalarials targeting haem detoxification pathway of malaria parasite.

引用

页码：487 / 494

页数：8

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