Browsing by Author "Bom, J"
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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.
- Imidazolidin-4-one derivatives of primaquine as novel transmission-blocking antimalarialsPublication . Araujo, MJ; Bom, J; Capela, R; Casimiro, C; Chambel, P; Gomes, P; Iley, J; Lopes, F; Morais, J; Moreira, R; de Oliveira, E; do Rosario, V; Vale, NImidazolidin-4-one derivatives of primaquine were synthesized as potential double prodrugs of the parent drug. The title compounds inhibit the development of the sporogonic cycle of Plasmodium berghei, affecting the appearance of oocysts in the midguts of the mosquitoes. The imidazolidin-4-ones are very stable, both in human plasma and in pH 7.4 buffer, indicating that they are active per se. Thus, imidazolidin-4-ones derived from 8-aminoquinolines represent a new entry in antimalarial structure-activity relationships.
- Search for active compounds from a medicinal plant used as antimalarial in S. Tomé and Príncipe islandsPublication . Mil-Homens, T; Duarte, N; Bom, J; Ferreira, I; Cravo, P; Madureira, MC; Ferreira, MJ