Journal
MOLECULES
Volume 22, Issue 5, Pages -Publisher
MDPI
DOI: 10.3390/molecules22050709
Keywords
anti-T. cruzi and anti-Leishmania spp. activity; arylidene ketones; thiazolidene hydrazines; triosephosphate isomerase; cruzipain; in vivo toxicity; zebrafish
Funding
- CSIC (Comision Sectorial de Investigacion Cientifica)
- Direccion General de Asuntos del Personal Academico-Universidad Nacional Autonoma de Mexico-Programa de Apoyo a Proyectos de Investigacion e Innovacion Tecnologica [IN206816]
- CONACyT-Mexico [254694]
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A series of fifty arylideneketones and thiazolidenehydrazines was evaluated against Leishmania infantum and Leishmania braziliensis. Furthermore, new simplified thiazolidenehydrazine derivatives were evaluated against Trypanosoma cruzi. The cytotoxicity of the active compounds on non-infected fibroblasts or macrophages was established in vitro to evaluate the selectivity of their anti-parasitic effects. Seven thiazolidenehydrazine derivatives and ten arylideneketones had good activity against the three parasites. The IC50 values for T. cruzi and Leishmania spp. ranged from 90 nM-25 mu M. Eight compounds had multi-trypanocidal activity against T. cruzi and Leishmania spp. (the etiological agents of cutaneous and visceral forms). The selectivity of these active compounds was better than the three reference drugs: benznidazole, glucantime and miltefosine. They also had low toxicity when tested in vivo on zebrafish. Trying to understand the mechanism of action of these compounds, two possible molecular targets were investigated: triosephosphate isomerase and cruzipain. We also used a molecular stripping approach to elucidate the minimal structural requirements for their anti-T. cruzi activity.
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