Synthesis and biological evaluation of new 1,4‐benzothiazine derivatives as potential COX‐2 inhibitors

A series of new 2H‐benzo[1,4]thiazine derivatives were synthesized from aroylmethylidene malonates and o‐aminothiophenols by condensation/cyclization methodology in order to evaluate their COX‐2 inhibitory activity. In‐silico studies indicated that among the synthesized compounds, 5i could serve as...

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Bibliographic Details
Published in:Journal of heterocyclic chemistry 2022-02, Vol.59 (2), p.351-358
Main Authors: Meenakshi, Maniarasu, Antojenifer, Panneerselvam, Karthikeyan, Muthusamy, Prahalathan, Chidambaram, Srinivasan, Kannupal
Format: Article
Language:English
Subjects:
COX-2 inhibitors
Synthesis
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Summary:A series of new 2H‐benzo[1,4]thiazine derivatives were synthesized from aroylmethylidene malonates and o‐aminothiophenols by condensation/cyclization methodology in order to evaluate their COX‐2 inhibitory activity. In‐silico studies indicated that among the synthesized compounds, 5i could serve as a potential candidate for the task. So, compound 5i was taken as a model ligand for in vitro studies. The favorable outcome of the studies showed that compound 5i is indeed an excellent inhibitor of COX‐2. Synthesis and biological evaluation of new 1,4‐benzothiazine derivatives as potential COX‐2 inhibitors
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.4389