
%0 Journal Article
%A Cowman,, Alan F. 
%A Deady,, Leslie W. 
%A Deharo,, Eric 
%A Desneves, José 
%A Tilley, Leann 
%T Synthesis and Activity of Some Antimalarial Bisquinolinemethanols
%J Australian Journal of Chemistry
%D 1998/01/13
%V 50
%N 11
%P 1091-1096
%K 
%R https://doi.org/10.1071/C97086
%U https://www.publish.csiro.au/paper/C97086 
%X 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&#8242;-hydroxy group by -(CH2)2n- bridges (n = 2-5) (series A), and six bis amides, from 8&#8242;-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 were compounds as active as mefloquine, with diminished cross-resistance to the mefloquine-resistant strain. The most potent (series B, n = 4) was highly active against chloroquine-sensitive, chloroquine-resistant and mefloquine-resistant parasites. Invivo testing, however, showed the compound to be too toxic for further development 
