In vitro, in silico and in vivo analysis of novel aromatic amidines against Trypanosoma cruzi [PublishAheadOfPrint]

Five bis-arylimidamides were assayed as anti-T.cruzi agents using in vitro, in silico and in vivo approaches. All were considered no PAINS, have favorable pharmacokinetic landscape, were active against trypomastigotes and intracellular forms but combined with benznidazole gave no interaction. The most selective (28SMB032) moved to in vivo led to 40% parasitemia reduction (0.1mg/kg/5 days by ip) but without mortality protection. In silico target fishing suggested DNA as main target, but ultrastructural data did not match.

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