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  • Title: SYNTHESIS, ANTIMICROBIAL, ANTICANCER EVALUATION AND QSAR STUDIES OF THIAZOLIDIN-4-ONE DERIVATIVES.
    Author: Deep A, Kumar P, Narasimhan B, Lim SM, Ramasamy K, Mishra RK, Mani V.
    Journal: Acta Pol Pharm; 2016; 73(1):93-106. PubMed ID: 27008804.
    Abstract:
    In this study, a novel series of 4-thiazolidinone derivatives (1-17) was synthesized and evaluated for its in vitro antimicrobial and anticancer potentials. N-(2-(5-(4-nitrobenzylidene)-2-(4-chlorophenyl)-4-oxothia- zolidin-3-ylamino)-2-oxoethyl) benzamide (7, pMICam = 1.86 µM/mL) was found to be the most active antimi- crobial agent. The anticancer study results demonstrated that N-(2-(5-(4-hydroxybenzylidene)-2-(4- methoxyphenyl)-4-oxothiazolidin-3-ylamino)-2-oxoethyl) benzamide (10, IC₅₀ = 18.59 µM) was the most active anticancer agent. QSAR studies indicated the importance of topological parameter, Kier's α third order shape index (κα₃) as well as electronic parameters, cosmic total energy (cos E) and energy of highest occupied molecular orbital (HOMO) in describing the antimicrobial activity of synthesized compounds.
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