In Vitro , In Silico , and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi
Year: 2017
Type: article
Abstract: ABSTRACT 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.
DOI: 10.1128/aac.02205-17
Authors: Camila C. Santos, Jéssica R. Lionel, Raiza B. Peres, Marcos M. Batista, Patrícia B. da Silva, Gabriel M. de Oliveira, Cristiane F. da Silva, Denise G. J. Batista, Sandra Maria O. Souza, Carolina H. Andrade, Bruno J. Neves, Rodolpho C. Braga, Donald A. Patrick, Svetlana M. Bakunova, Richard R. Tidwell, Maria de Nazaré C. Soeiro
Language: English
Subfield: Epidemiology
Field: Medicine
Domain: Health Sciences
Open Access status: bronze
OpenAlex ID: W2932829808