4 documents found, page 1 of 1
Medicinal Chemistry
Moreira, R; Carreiras, MC; Lopes, F; Rocha, MJP; Mendes, E; LConstantino, Dias,; Santos, MM; Lavrado, J; Capela, R; Santana, AB; Valente, E
Imidazolidin-4-one derivatives of primaquine as novel transmission-blocking ant...
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...
Imidazolidin-4-one derivatives of primaquine as novel transmission-blocking ant...
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...
Amidomethylation of amodiaquine
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...