Author/Authors :
Lopes، نويسنده , , Francisca and Capela، نويسنده , , Rita and Gonçaves، نويسنده , , José O. and Horton، نويسنده , , Peter N. and Hursthouse، نويسنده , , Michael B. and Iley، نويسنده , , Jim and Casimiro، نويسنده , , Catarina M. and Bom، نويسنده , , Joana and Moreira، نويسنده , , Rui، نويسنده ,
Abstract :
Novel N-Mannich base-type derivatives of the antimalarial drug amodiaquine were synthesised by reaction with tertiary N-chloromethylamides. With the exception of the derivative of ethyl hippurate, all the so-formed (1-amidomethyl-1H-quinolin-4-ylidene)arylamines displayed high chemical and enzymatic stability. These compounds displayed antimalarial activity against the multi-drug resistant Plasmodium falciparum strain Dd2 (IC50 values 15–31 nM) and demonstrated no significant loss in activity compared to amodiaquine (IC50 30 nM).
