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Recent developments in trans-sialidase inhibitors of Trypanosoma cruzi

Authors :
Edgar E. Lara-Ramírez
Muhammad Ashfaq
Esther Ramírez-Moreno
Gildardo Rivera
Virgilio Bocanegra-García
Antonio Moreno-Herrera
Muhammad Kashif
Source :
Journal of drug targeting. 25(6)
Publication Year :
2017

Abstract

Chagas is a lethal chronic disease that currently affects 8–10 million people worldwide, primarily in South and Central America. Trypanosoma cruzi trans-sialidase is an enzyme that is of vital importance for the survival of the parasite due to its key role in the transfer of sialic acid from the host to the parasite surface and it also helps the parasite combat the host’s immune system. This enzyme has no equivalent human enzyme; thus, it has become an interesting target for the development of inhibitors that combat the parasite. In this review, we summarize three classes of inhibitors (acceptor, donor and unrelated) with their inhibition values and their mode of action against this enzyme. Based on molecular docking, molecular dynamics and structure-activity relationship studies, it has been discovered that the molecules with –NH2, –OH and –COOH groups on an aromatic ring could be used as a scaffold for the development of new and potent trans-sialidase inhibitors due to their key interaction with...

Details

ISSN :
10292330
Volume :
25
Issue :
6
Database :
OpenAIRE
Journal :
Journal of drug targeting
Accession number :
edsair.doi.dedup.....0c7440a33a9a6fbace2cecec3e8813b6