SYNTHESIS AND DOCKING STUDIES OF 2-(NITROOXY)-ETHYL-2-(SUBSTITUTED-2,5-DIPHENYL-OXAZOLE)-ACETATE AS ANTI-INFLAMMATORY AGENTS WITH ANALGESIC AND NITRIC OXIDE RELEASING PROPERTIES
Keywords:
Oxazole, Docking, Anti-inflammatory, Analgesic, Nitric oxideAbstract
Objective: The objective of the reported study was to develop new chemical entities as potential anti-inflammatory agents with analgesic and nitric oxide releasing properties.
Methods: The compounds were designed with the help of docking studies. In the synthetic study the target compounds were obtained by reacting 2-(substituted-2,5-diphenyl-oxazole)-acetic acid (2a-2v) with nitro-oxy ethyl bromide in the presence of dimethyl formamide and potassium carbonate to give 2-(nitrooxy) ethyl 2-(substituted-2,5-diphenyl-oxazole) acetate derivatives (3a-3v). The synthesized derivatives were characterized with the help of different analytical techniques and further evaluated for anti-inflammatory, analgesic and nitric oxide releasing activity.
Results: With the help of docking study it was proven that compounds 3a, 3c, 3g, 3l and 3r showed significant G-score. In the anti-inflammatory and analgesic study also, compounds 3a, 3c, 3g, 3l and 3r exhibited promising activity. All the synthesized compounds exhibited significant nitric oxide releasing properties both in-vitro and in-vivo.
Conclusion: Compounds 3a, 3c, 3g, 3l and 3r exhibited prominent anti-inflammatory and analgesic activity.
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