Journal article

Synthesis and activity of some antimalarial bisquinolinemethanols

AF Cowman, LW Deady, E Deharo, J Desneves, L Tilley

AUSTRALIAN JOURNAL OF CHEMISTRY | CSIRO PUBLISHING | Published : 1997

Abstract

A new type of bisquinoline antimalarial, containing the basic side chain of the cinchona alkaloids, has been evaluated. Five bis ethers, from 10,11-dihydrocupreine linked through the 6′-hydroxy group by -(CH2)2n- bridges (n = 2-5) (series A), and six bis amides, from 8′-amino-10,11-dihydrocinchonidine linked by -CO(CH2)2nCO- bridges (n = 1-6) (series B), were synthesized and screened against chloroquine-sensitive and -resistant strains and a mefloquine-resistant strain of Plasmodium falciparum in vitro. Two analogues of series B (n = 4, 5), with a 2-(dibutylamino)-1-hydroxyethyl side chain (series C), were also included. Compounds within series A were generally least active. Among the rest w..

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