Chagas disease and leishmaniasis are neglected tropical diseases with limited treatment options. This study reports a hit‐to‐lead optimization of morpholinephenylbenzamides, starting from hit 1, which showed potent activity against Trypanosoma cruzi (IC50 0.29–0.76 μM) and Leishmania infantum (IC50 10.7 μM), despite a...
D. Farago, Daniela de Melo Resende, Mariza Gabriela Faleiro de Moura Lodi Cruz et al.· ChemMedChem· 0 citations
In vitro investigation of Benzenesulfonylpiperazines 2 revealed that it exerts a cytostatic effect on Leishmania infantum promastigotes, promoting cell cycle arrest during the G0/G1 phase which may potentially be linked to the production of reactive oxygen species.
Thibault Joseph William Jacques Dit Lapierre, Mariza Gabriela Faleiro de Moura Lodi Cruz, Guilherme Freitas de Lima Hercos et al.· Chemical Biology and Drug De...· 0 citations
Overall, this work establishes compound 1 as a promising hit for congenital toxoplasmosis and malaria, providing a clear roadmap for future hit-to-lead optimization to overcome its current pharmacokinetic limitations.
J. O. Carvalho, Ana Paula C. Procópio, M. P. O. Almeida et al.· Journal of the Brazilian Che...· 0 citations
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