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Synthesis, antiamoebic and molecular docking studies of furan-thiazolidinone hybrids

Authors :
Mohammad Fawad Ansari
Samudrala Gourinath
Shadab Miyan Siddiqui
Sudhaker Dharavath
Kamal Ahmad
Fernando Avecilla
Amir Azam
Source :
European Journal of Medicinal Chemistry. 124:393-406
Publication Year :
2016
Publisher :
Elsevier BV, 2016.

Abstract

In continuation of our previous work, a series of furan-thiazolidinone hybrids was prepared by Knoevenagel condensation of 3-(furan-2-ylmethyl)-2-(phenylimino)-1, 3-thiazolidin-4-one with different aryl aldehydes in presence of strong base. Some members of the series exhibited remarkable antiamoebic activity and cell viability. Three compounds (3, 6 and 11) showed excellent binding energy for Entamoeba histolytica O-acetyle-l-serine sulfohydrolase and Entamoeba histolytica thioredoxin reductase. These compounds demonstrated significant inhibition of O-acetyle-l-serine sulfohydrolase. The promising antiamoebic activity and enzymatic assay of 3, 6 and 11 make them promising molecules for further lead optimization in the development of novel antiamoebic agents.

Details

ISSN :
02235234
Volume :
124
Database :
OpenAIRE
Journal :
European Journal of Medicinal Chemistry
Accession number :
edsair.doi.dedup.....09a3dfb1f81a45a9eaab87d9c91e787f
Full Text :
https://doi.org/10.1016/j.ejmech.2016.08.053