Literature DB >> 29141568

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.

Aniket P Sarkate1, Deepak K Lokwani2, Kshipra S Karnik1, Devanand B Shinde3.   

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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Entities:  

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

Mesh:

Substances:

Year:  2017        PMID: 29141568     DOI: 10.2174/1871523016666171115125922

Source DB:  PubMed          Journal:  Antiinflamm Antiallergy Agents Med Chem        ISSN: 1871-5230


  2 in total

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Authors:  Ewa Żesławska; Robert Zakrzewski; Arkadiusz Nowicki; Izabela Korona-Głowniak; Antonín Lyčka; Agnieszka Kania; Krzysztof Kazimierz Zborowski; Piotr Suder; Agnieszka Skórska-Stania; Waldemar Tejchman
Journal:  Molecules       Date:  2022-06-21       Impact factor: 4.927

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Authors:  Jhana O Hendrickx; Wim Martinet; Debby Van Dam; Guido R Y De Meyer
Journal:  Front Mol Biosci       Date:  2021-03-29
  2 in total

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