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Bioorg Med Chem ; 11(18): 4083-91, 2003 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-12927870

RESUMO

During the course of a collaborative screening program, a set of 1-phenyl-4-pyridyl-butadienes was found to exhibit in vitro activity against Eimeria tenella in a cell-based assay. Activity was dependent on the chain length and degree of unsaturation of the linker between the two aryl groups as well as substitution of the pyridine moiety. Structure-activity relationship studies were subsequently conducted over a larger range of 1,4-diarylbutadienes in order to determine the scope of active compounds, to identify structural patterns governing activity and to enhance in vitro potency against E. tenella. In addition, the efficacy of many compounds for treating coccidiosis in chickens was measured by testing the ability of the compound to prevent or reduce intestinal and cecal lesions when administered by oral gavage. A few compounds in the series were identified that exhibited a moderate degree of in vitro and in vivo activity.


Assuntos
Antiprotozoários/síntese química , Butadienos/síntese química , Eimeria tenella/efeitos dos fármacos , Animais , Antiprotozoários/farmacologia , Butadienos/farmacologia , Butadienos/toxicidade , Células Cultivadas , Galinhas , Coccidiose/tratamento farmacológico , Coccidiose/veterinária , Avaliação Pré-Clínica de Medicamentos , Técnicas In Vitro , Nitroimidazóis/química , Nitroimidazóis/farmacologia , Doenças das Aves Domésticas/tratamento farmacológico , Relação Estrutura-Atividade
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