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.
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.
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