Novel 2-(nitrooxy)ethyl 2-(4-(substituted phenyl)-2-((substituted phenyl)amino)thiazol-5-yl)acetate as Anti-inflammatory, Analgesic and Nitric Oxide Releasing Agents: Synthesis and Molecular Docking Studies

Author(s): Aniket P. Sarkate* , Deepak K. Lokwani , Kshipra S. Karnik , Devanand B. Shinde .

Journal Name: Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry

Volume 16 , Issue 3 , 2017

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Abstract:

Background: Due to the need and adverse effects associated with the available anti-inflammatory agents, an attempt was made to develop the new anti-inflammatory agents with better activity and lesser adverse effects.

Objective: Synthetic approaches based on chemical modification of NSAIDs have been undertaken with the aim of improving NSAIDs safety profile.

Method: In the present study, a series of thiazole derivatives (3a-3x) was synthesized and tested for its anti-inflammatory with analgesic and nitric oxide releasing properties. In this work, synthesis of molecules containing substituted diaryl ring on 5-membered thiazole ring with nitric oxide releasing moiety is described.

Results: Out of the twenty four synthesized compounds, five compounds showed considerable anti-inflammatory and analgesic activity in comparison with the standard. Most of the synthesized compounds showed considerable nitric oxide-releasing property. The molecular docking study was used to rationalize binding interaction at the active site and the result showed good binding interaction.

Conclusion: From the results of pharmacological studies, we conclude that the synthesized compounds have not only retained, but showed enhanced anti-inflammatory and analgesic profile.

Keywords: Analgesic, anti-inflammatory, binding interaction, docking, nitric oxide, thiazole.

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Article Details

VOLUME: 16
ISSUE: 3
Year: 2017
Page: [153 - 167]
Pages: 15
DOI: 10.2174/1871523016666171115125922
Price: $58

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