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http://hdl.handle.net/10451/21194| Título: | Amidomethylation of amodiaquine antimalarial N-Mannich base derivatives |
| Autor: | Lopes, F Capela, R Goncaves, JO Horton, PN Hursthouse, MB Iley, J Casimiro, CM Bom, J Moreira, R |
| Palavras-chave: | Chemistry, Organic |
| Data: | 2004 |
| Editora: | PERGAMON-ELSEVIER SCIENCE LTD |
| Citação: | TETRAHEDRON LETTERS. - Vol. 45, n. 41 (OCT 4 2004), p. 7663-7666 |
| Resumo: | 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 30nM). (C) 2004 Elsevier Ltd. All rights reserved. |
| URI: | http://hdl.handle.net/10451/21194 |
| DOI: | http://dx.doi.org/10.1016/j.tetlet.2004.08.093 |
| ISSN: | 0040-4039 |
| Aparece nas colecções: | FF - Produção Científica 2000-2009 |
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