Systematic search for benzimidazole compounds and derivatives with antileishmanial effects

Molecular Diversity
Juan Carlos Sánchez-SalgadoYareli Rojas-Aguirre

Abstract

Leishmaniasis is a neglected tropical disease that currently affects 12 million people, and over 1 billion people are at risk of infection. Current chemotherapeutic approaches used to treat this disease are unsatisfactory, and the limitations of these drugs highlight the necessity to develop treatments with improved efficacy and safety. To inform the rational design and development of more efficient therapies, the present study reports a chemoinformatic approach using the ChEMBL database to retrieve benzimidazole as a target scaffold. Our analysis revealed that a limited number of studies had investigated the antileishmanial effects of benzimidazoles. Among this limited number, L. major was the species most commonly used to evaluate the antileishmanial effects of these compounds, whereas L. amazonensis and L. braziliensis were used least often in the reported studies. The antileishmanial activities of benzimidazole derivatives were notably variable, a fact that may depend on the substitution pattern of the scaffold. In addition, we investigated the effects of a benzimidazole derivative on promastigotes and amastigotes of L. infantum and L. amazonensis using a novel fluorometric method. Significant antileishmanial effects were o...Continue Reading

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Citations

Apr 12, 2019·American Journal of Human Biology : the Official Journal of the Human Biology Council·María P Redondo-Del-RíoBeatriz de-Mateo-Silleras
Nov 26, 2019·Current Pharmaceutical Design·Jéssika de Oliveira VianaMarcus Tullius Scotti
Nov 9, 2019·SAR and QSAR in Environmental Research·S KapilO Silakari
May 15, 2021·Frontiers in Chemistry·Crhisllane Rafaele Dos Santos Vasconcelos, Antonio Mauro Rezende
Jun 26, 2021·European Journal of Medicinal Chemistry·Ojasvi GuptaVikramdeep Monga

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Methods Mentioned

BETA
light microscopy

Software Mentioned

MEQI
Molecular Equivalence Indices ( MEQI )
LCS
SPSS
ChEMBL

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