1. Synthesis, antiamoebic and molecular docking studies of furan-thiazolidinone hybrids.
- Author
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Ansari MF, Siddiqui SM, Ahmad K, Avecilla F, Dharavath S, Gourinath S, and Azam A
- Subjects
- Animals, Antiprotozoal Agents chemical synthesis, Antiprotozoal Agents metabolism, Antiprotozoal Agents pharmacokinetics, Antiprotozoal Agents pharmacology, CHO Cells, Cell Survival drug effects, Chemistry Techniques, Synthetic, Cricetinae, Cricetulus, Entamoeba histolytica enzymology, Inhibitory Concentration 50, Protein Conformation, Structure-Activity Relationship, Thiazolidines metabolism, Thiazolidines pharmacokinetics, Thioredoxin-Disulfide Reductase antagonists & inhibitors, Thioredoxin-Disulfide Reductase chemistry, Thioredoxin-Disulfide Reductase metabolism, Drug Design, Entamoeba histolytica drug effects, Furans chemistry, Molecular Docking Simulation, Thiazolidines chemical synthesis, Thiazolidines pharmacology
- 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., (Copyright © 2016. Published by Elsevier Masson SAS.)
- Published
- 2016
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