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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.
- Source :
-
Anti-inflammatory & anti-allergy agents in medicinal chemistry [Antiinflamm Antiallergy Agents Med Chem] 2017; Vol. 16 (3), pp. 153-167. - Publication Year :
- 2017
-
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.<br />Objective: Synthetic approaches based on chemical modification of NSAIDs have been undertaken with the aim of improving NSAIDs safety profile.<br />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.<br />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.<br />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.<br /> (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)
- Subjects :
- Acetates therapeutic use
Analgesics therapeutic use
Animals
Anti-Inflammatory Agents therapeutic use
Carrageenan
Edema chemically induced
Female
Humans
Male
Mice
Molecular Docking Simulation
Nitric Oxide metabolism
Rats
Rats, Wistar
Structure-Activity Relationship
Thiazoles therapeutic use
Acetates chemistry
Analgesics chemistry
Anti-Inflammatory Agents chemistry
Anti-Inflammatory Agents, Non-Steroidal chemistry
Chemistry, Pharmaceutical methods
Edema drug therapy
Thiazoles chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1875-614X
- Volume :
- 16
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Anti-inflammatory & anti-allergy agents in medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 29141568
- Full Text :
- https://doi.org/10.2174/1871523016666171115125922