2024-11-182024-11-182017SANTOS, Camila C. et al. In vitro, in silico and in vivo analysis of novel aromatic amidines against Trypanosoma cruzi. Antimicrobial Agents and Chemotherapy, Washington, v. 62, n. 2, e02205-17, 2017. DOI: 10.1128/AAC.02205-17. Disponível em: https://journals.asm.org/doi/10.1128/aac.02205-17?url_ver=Z39.88-2003&rfr_id=ori%3Arid%3Acrossref.org&rfr_dat=cr_pub++0pubmed. Acesso em: 11 nov. 2024.0066-4804e- 1098-6596http://repositorio.bc.ufg.br//handle/ri/25883Five 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.engAcesso Abertohttp://creativecommons.org/licenses/by-nc-nd/4.0/Chagas diseaseArylimidamidesExperimental chemotherapyIn vivoArtigo10.1128/AAC.02205-17