Publications by authors named "Daniela Gaspar-Silva"

Article Synopsis
  • Current treatments for leishmaniasis have high toxicity and failure rates, highlighting the need for new, less toxic drugs.
  • A study tested several sulfonamide 4-methoxychalcone derivatives for their effectiveness against L. amazonensis and found that compound 3f showed the best results with low toxicity, while compound 3i was more effective against L. braziliensis.
  • Molecular modeling revealed that factors like molecular volume and electron density play a role in the effectiveness of these compounds, suggesting they could lead to new treatment options for leishmaniasis.
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Despite clinical importance of leishmaniasis, an infectious disease that affects 12 thousand million people in 88 countries, the treatment is still unsatisfactory due to its limited efficacy, cost expensive and undesirable side effects. Aiming to develop new antileishmanial lead compounds, we used a rational approach to synthesize a new set of sulfonamide 4-methoxychalcone derivatives (3a-3i) and evaluate the sulfonamide and methoxy moieties as promising adding-groups to chalcones. For that purpose we tested this new set against Leishmania braziliensis promastigotes and intracellular amastigotes and determined its cell toxicity profile.

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In the present paper 12 N-quinolin-8-yl-arylsulfonamides synthesized by coupling 8-aminoquinolines with various arylsulfonylchlorides were assayed in vitro against Leishmania amazonensis, Leishmania chagasi and Trypanosoma cruzi strains. This series of new compounds were found to be selective for Leishmania spp. promastigote and amastigote forms.

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