Browsing by Author "Casimiro, CM"
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- Amidomethylation of amodiaquinePublication . Lopes, F; Capela, R; Goncaves, JO; Horton, PN; Hursthouse, MB; Iley, J; Casimiro, CM; Bom, J; Moreira, RNovel 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 30nM). (C) 2004 Elsevier Ltd. All rights reserved.