African Journal of
Pharmacy and Pharmacology

  • Abbreviation: Afr. J. Pharm. Pharmacol.
  • Language: English
  • ISSN: 1996-0816
  • DOI: 10.5897/AJPP
  • Start Year: 2007
  • Published Articles: 2288

Full Length Research Paper

Synthesis, in-vitro, in-vivo evaluation and molecular docking of 2-(3-(2-(1, 3-dioxoisoindolin-2-yl) acetamido)-4-oxo-2-substituted thiazolidin-5-yl) acetic acid derivatives as anti-inflammatory agents

Anna Pratima Nikalje*
  • Anna Pratima Nikalje*
  • Department of Pharmaceutical Chemistry, Y.B. Chavan College of Pharmacy, Dr. Rafiq Zakaria Campus, Rauza Bagh, P.B. No. 33, Aurangabad-431001, Maharashtra, India.
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Nazma Hirani
  • Nazma Hirani
  • Department of Pharmacology, Y.B. Chavan College of Pharmacy, Dr. Rafiq Zakaria Campus, Rauza Bagh, P.B. No. 33, Aurangabad-431001, Maharashtra, India.
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R. Nawle
  • R. Nawle
  • Department of Pharmacology, Government College of Pharmacy, Aurangabad-431001, Maharashtra, India.
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  •  Received: 30 December 2014
  •  Accepted: 21 January 2015
  •  Published: 22 February 2015

Abstract

A series of novel 2-(3-(2-(1,3-dioxoisoindolin-2-yl) acetamido)-4-oxo-2-phenylthiazolidin-5-yl) acetic acid (5a-l) have been synthesized by cyclocondensation of N-substituted benzylidene/methylene-2-(1,3-dioxo isoindolin-2-yl) acetohydrazide (4a-l) with mercapto succinic acid in dimethylformamide (DMF) as solvent and using anhydrous zinc chloride as a catalyst in microsynth microwave reactor. The synthesized compounds were evaluated for anti-inflammatory activity using in vitro and in vivo model. Furthermore, ulcerogenic toxicity study was performed for selected compounds. All the compounds have shown promising anti-inflammatory activity in both the models. Docking studies were performed to know the binding affinity towards the human serum albumin (HSA).

Key words: Thiazolidinone, microwave assisted, anti-inflammatory, protein denaturation, rat paw edema, molecular docking.

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This article is published under the terms of the Creative Commons Attribution License 4.0

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