Antimicrobial Agents and Chemotherapy · 2017 · 23 citations · 24 references
Five bis-arylimidamides were assayed as anti-<i>Trypanosoma cruzi</i> agents by <i>in vitro</i>, <i>in silico</i>, and <i>in vivo</i> 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 <i>in vivo</i> led to a 40% reduction in parasitemia (0.1 mg/kg of body weight/5 days intraperitoneally) but without mortality protection. <i>In silico</i> target fishing suggested DNA as the main target, but ultrastructural data did not match.
24