Research Publications

Back

SYNTHESIS AND ACTIVITY OF SOME ANTIMALARIAL BISQUINOLINES


RAYNES, K; Galatis, D; Cowman, AF; Tilley, L; Deady, LW
1995-01-06
JOURNAL OF MEDICINAL CHEMISTRY
Journal Article
38
1
204-206
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.
AMER CHEMICAL SOC
PLASMODIUM-FALCIPARUM; CHLOROQUINE; RESISTANCE; MALARIA; GENE
10.1021/jm00001a026
Refer to copyright notice on published article.

Back
Creation Date 1995-01-06 12:00:00