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Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry


ISSN (Print): 1871-5230
ISSN (Online): 1875-614X

Research Article

Discovery of Thiazole Based Bis Heterocyclic System for Anti- Inflammatory Potential

Author(s): Amit S. Tapkir, Sohan S. Chitlange* and Ritesh P. Bhole

Volume 16, Issue 3, 2017

Page: [175 - 192] Pages: 18

DOI: 10.2174/1871523016666171114165958

Price: $65


Background: We have developed a new series of 36 substituted thiazole derivatives prepared via reaction of substituted benzothiazole-2-amine with substituted phenacyl bromide.

Objective: This study was aimed to develop and successfully evaluate anti-inflammatory activity of substituted thiazole derivatives.

Method: A new series of 36 substituted thiazole derivatives was synthesized and derivatives were characterized by analytical and spectrometric methods like IR, MS, and 1H NMR. The molecular docking was performed for all the synthesized thiazole derivatives to assess their binding affinities to COX-2 isozyme. The best compounds from docking study were subjected for their anti-inflammatory activity by using rat hind paw edema method.

Results: Results from carrageenan-induced hind paw edema showed that compounds 3h, 5a, 5e, 9d, and 9h possess significant anti-inflammatory activity. The result from vascular permeability indicating inhibition of vascular permeability with compounds 3h and 9h is significant and results from cotton pellet granuloma formation models show greater degree of inhibition with compounds 3h and 5a to contribute to their significant anti-inflammatory activity.

Conclusion: This study provides successful development of novel thiazole derivatives. Their binding affinities to COX-2 enzyme were also confirmed, indicating that developed molecules are comparable to diclofenac and hence could be promising anti-inflammatory agents.

Keywords: Anti-inflammatory activity, benzothiazoles, bis-heterocycles, COX, thiazole.

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