期刊
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
卷 62, 期 2, 页码 -出版社
AMER SOC MICROBIOLOGY
DOI: 10.1128/AAC.02205-17
关键词
Chagas disease; arylimidamides; experimental chemotherapy; in vivo
资金
- Fundacao Carlos Chagas Filho de Amparo a Pesquisa do Estado do Rio de Janeiro (FAPERJ)
- Conselho Nacional Desenvolvimento Cientifico e Tecnologico (CNPq)
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES)
- Fundacao Oswaldo Cruz
- PDTIS
- PAEF/CNPq/Fiocruz
- CAPES
- Fortalecimento dos Programas de Gestao Estrategica de Pesquisa da Fiocruz Rede de Plataformas Fiocruz [VPPLR-001-Fio 14]
Five bis-arylimidamides were assayed as anti-Trypanosoma cruzi agents by in vitro, in silico, and in vivo approaches. None were considered to be pan-assay interference compounds. They had a favorable pharmacokinetic landscape and were active against trypomastigotes and intracellular forms, and in combination with benznidazole, they gave no interaction. The most selective agent (28SMB032) tested in vivo led to a 40% reduction in parasitemia (0.1 mg/kg of body weight/5 days intraperitoneally) but without mortality protection. In silico target fishing suggested DNA as the main target, but ultrastructural data did not match.
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