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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

[ Vol. 16 , Issue. 3 ]


Aniket P. Sarkate*, Deepak K. Lokwani, Kshipra S. Karnik and Devanand B. Shinde   Pages 153 - 167 ( 15 )


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


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


Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad- 431004, MS, Department of Pharmaceutical Chemistry, R.C. Patel Institute of Pharmaceutical Education & Research, Shirpur-425405, MS, Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad- 431004, MS, Shivaji University, Vidyanagar, Kolhapur-416004, MS

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