Volume 3, Issue 8


Synthesis, Characterization and in vitro and in vivo evaluation of anti-inflammatory activity of some novel 4-Thiazolidinone derivatives

Author: Asish Bhaumik, M. Upender Kumar, Kaleem Ahmed Khan, Ch. Srinivas, Sujay Sharma

Abstract: The objective of the present work was the synthesis of N-[2-(4-substituted phenyl)-4-oxo-1,3-thiazolidine-3-yl]-2-(naphthalene-2-yloxy)acetamide and evaluation of in-vitro anti-inflammatory activity by Molecular Docking against COX II enzyme as well as in vivo by carrageen an induced paw edema method in rats. Based on this a new series of compound had been planned to synthesize by reacting β-naphthol, ethyl chloroacetate, hydrazinemonohydrate, ethylalcohol and various aromatic aldehydes in presence of anhydrous potassium carbonate The synthesized compounds were characterized by IR, NMR, and Mass spectroscopy. In vitro molecular docking had shown that the estimated inhibition constant of the compound A9, A4, A6, A10, A5 and A8 were found to be 1.55 mM, 1.45 uM, 116.4 uM, 454.39 uM, 454.39 uM and 35.84 mM. So these six compounds possessed pronounced anti-inflammatory activity which were evaluated on the basis of free energy binding (K.cal/mol), vdw+H-bonding + dissolved energy (K.cal/ml),electrostatic energy and total intermolecular energy (K.cal/mol) which were involved in the therapeutic efficacy of the new drug molecules. In vivo anti-inflammatory activity displayed that the above six synthesized compounds exhibited a good anti-inflammatory activity among the ten synthesized compounds and had percentage protection compound A9(% of protection 68.9), A4((% of protection 68.5), A6((% of protection 60.5), A10(% of protection58.54), A5((% of protection56.24), and A8((% of protection 52.05).


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