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Amidomethylation of amodiaquine: antimalarial N-Mannich base derivatives

Lopes, Francisca; Capela, Rita; Gonçaves, Jose O.; Horton, Peter N.; Hursthouse, Michael B.; Iley, Jim; Casimiro, Catarina M.; Bom, Joana and Moreira, Rui (2004). Amidomethylation of amodiaquine: antimalarial N-Mannich base derivatives. Tetrahedron Letters, 45(41) 7663 -7666.

DOI (Digital Object Identifier) Link: http://dx.doi.org/10.1016/j.tetlet.2004.08.093
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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 15–31nM) and demonstrated no significant loss in activity compared to amodiaquine (IC50 30nM).

Item Type: Journal Article
Copyright Holders: 2004 Elsevier Ltd.
ISSN: 0040-4039
Keywords: amodiaquine; malaria; Mannich basel; Amodiaquine; Amidomethylation; antimalarial
Academic Unit/Department: Science > Life, Health and Chemical Sciences
Item ID: 3989
Depositing User: James Iley
Date Deposited: 04 Jul 2006
Last Modified: 25 Jul 2011 15:01
URI: http://oro.open.ac.uk/id/eprint/3989
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