SYNTHESIS AND ACTIVITY OF SOME ANTIMALARIAL BISQUINOLINES

被引：67

作者：

RAYNES, K

GALATIS, D

COWMAN, AF

TILLEY, L

DEADY, LW

机构：

[1] LA TROBE UNIV,SCH CHEM,BUNDOORA,VIC 3083,AUSTRALIA

[2] LA TROBE UNIV,SCH BIOCHEM,BUNDOORA,VIC 3083,AUSTRALIA

[3] WALTER & ELIZA HALL INST MED RES,PARKVILLE,VIC 3052,AUSTRALIA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1995年 / 38卷 / 01期

关键词：

D O I：

10.1021/jm00001a026

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new type of bisquinoline antimalarial, in which the basic side chain of chloroquine is retained, has been evaluated. Nine bisamides were prepared from aliphatic diacids with 6-amino- and 8-amino-((4-(4-(diethylamino)-1-methylbutyl)amino)quinoline, and screened against chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. The resistance indices for all compounds were lower than for chloroquine. The position of attachment and length of the linker chain markedly affected activity. The most active (IC50 = 120 nM against the chloroquine-resistant FAC8 strain) was the -(O)C(CH2)(4)C(O)- linked 8-amino compound.

引用

页码：204 / 206

页数：3

共 13 条

[1] SELECTION FOR HIGH-LEVEL CHLOROQUINE RESISTANCE RESULTS IN DEAMPLIFICATION OF THE PFMDR1 GENE AND INCREASED SENSITIVITY TO MEFLOQUINE IN PLASMODIUM-FALCIPARUM [J].