DESIGN, FACILE SYNTHESIS, AND BIOLOGICAL EVALUATION OF NOVEL 1,3-THIAZINE DERIVATIVES AS POTENTIAL ANTICONVULSANT AGENTS
DOI:
https://doi.org/10.22159/ajpcr.2016.v9i5.13676Abstract
Objective: Chalcones and their heterocyclic analogs represent an important class of small molecules having anticonvulsant activities. Therefore, in
this study, the synthesis and anticonvulsant activity of some new chalcones and 1,3-thiazines were described.
Methods: The reaction of 1-acetylnaphthalene with substituted aromatic aldehydes in the presence of aq. NaOH afforded corresponding chalcones
which upon further cyclization with thiourea resulted in 1,3-thiazine derivatives. The newly synthesized compounds were tested for anticonvulsant
activity by pentylenetetrazole-induced seizures method using diazepam as standard.
Results: Most of the compounds showed good anticonvulsant activity but is less than diazepam. 1,3-thiazines were more potent than chalcones
and among them, compound P4 containing 4-fluorophenyl substituents on the thiazine moiety was more potent as it has prolonged the onset of
convulsions by 155.2 seconds.
Conclusion: We described the synthesis and anticonvulsant activity of novel chalcones and 1,3-thiazine derivatives. 1,3-thiazines are more active
anticonvulsant agents than chalcones and in particular compounds with electron withdrawing substituents.
Keywords: Chalcone, 1,3-thiazine, Pentylenetetrazole.
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