SYNTHESIS AND ACTIVITY OF SOME ANTIMALARIAL BISQUINOLINES
- Author(s)
- RAYNES, K; Galatis, D; Cowman, AF; Tilley, L; Deady, LW;
- Details
- Publication Year 1995-01-06,Volume 38,Issue #1,Page 204-206
- Journal Title
- JOURNAL OF MEDICINAL CHEMISTRY
- Publication Type
- Journal Article
- Abstract
- 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.
- Publisher
- AMER CHEMICAL SOC
- Keywords
- PLASMODIUM-FALCIPARUM; CHLOROQUINE; RESISTANCE; MALARIA; GENE
- Publisher's Version
- https://doi.org/10.1021/jm00001a026
- Terms of Use/Rights Notice
- Refer to copyright notice on published article.
Creation Date: 1995-01-06 12:00:00