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  • Title: Synthesis, antiamoebic and molecular docking studies of furan-thiazolidinone hybrids.
    Author: Ansari MF, Siddiqui SM, Ahmad K, Avecilla F, Dharavath S, Gourinath S, Azam A.
    Journal: Eur J Med Chem; 2016 Nov 29; 124():393-406. PubMed ID: 27597415.
    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.
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