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4-(1H-PYRAZOL-1-YL) BENZENESULFONAMIDE DERIVATIVES: IDENTIFYING NEW ACTIVE ANTILEISHMANIAL STRUCTURES FOR USE AGAINST A NEGLECTED DISEASE
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Abstract
Leishmaniasis is a neglected disease responsible for about 56,000 deaths every
year. Despite its importance, there are no effective, safe and proper treatments for
leishmaniasis due to strain resistance and/or drug side-effects. In this work we report the
synthesis, molecular modeling, cytotoxicity and the antileishmanial profile of a series of
4-(1H-pyrazol-1-yl)benzenesulfonamides. Our experimental data showed an active profile
for some compounds against Leishmania infantum and Leishmania amazonensis. The
profile of two compounds against L. infantum was similar to that of pentamidine, but with lower cytotoxicity. Molecular modeling evaluation indicated that changes in electronic
regions, orientation as well as lipophilicity of the derivatives were areas to improve the
interaction with the parasitic target. Overall the compounds represent feasible prototypes
for designing new molecules against L. infantum and L. amazonensis.
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