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
Investigation of the safety and therapeutic potential of (2E,5E)-2,5-bis(isoquinolin-5-ylmethylene)cyclopentanone (ICP) against Leishmania infantum indicates that it represents an interesting chemical scaffold for further optimization and investigation toward the development of new treatments for leishmaniasis.
Isabela Cristina Soares Martins, T. T. Santos, C. Queiroz-Junior et al.· Acta Tropica· 0 citations
It is demonstrated that GAT3 is a non-essential glycosomal ABC transporter that contributes to antileishmanial drug susceptibility in L. infantum and the association between GAT3 deletion and reduced expression of AQP1 and MT suggests a previously unrecognized link between glycosomal transport processes and pathways in...
H. M. Costa-Silva, Davi Alvarenga Lima, Lisandra Chieza Souza et al.· Parasitology international· 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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