
TY  - JOUR
A1  - Cowman,, Alan F. 
A1  - Deady,, Leslie W. 
A1  - Deharo,, Eric 
A1  - Desneves, José 
A1  - Tilley, Leann 
T1  - Synthesis and Activity of Some Antimalarial Bisquinolinemethanols
JF  - Australian Journal of Chemistry
JO  - Aust. J. Chem.
Y1  - 1998
VL  - 50
IS  - 11
SP  - 1091
EP  - 1096
KW  - 
UR  - https://doi.org/10.1071/C97086 
N2  - 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 
ER  -

