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Synthesis, Characterization and Biological Evaluation of Some Novel Substituted 1, 3-Thaizine Derivatives


Affiliations
1 Department of Pharmaceutical Chemistry, Vignan Institute of Pharmaceutical Sciences, Near Ramoji Film City, Deshmukhi, Nalgonda, Telangana-508284, India
     

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Thiazine derivatives are an important class of heterocyclic compounds and reported to possess a wide spectrum of biological properties. Thiazines exerted important anticonvulsant activity in models of generalized seizure which were well documented in the literature and therefore new thiazines were synthesized with an aim to get potent anticonvulsant agents. 4-methyl Cyclohexanone on Claisen-Schmidt condensation with various aromatic aldehydes in presence of dilute sodium hydroxide afforded the corresponding 2,6-disubstitutedarylidene cyclohexanones. Further these compounds were subjected to cyclocondensation with thiourea, catalyzed by aqueous potassium hydroxide to form 4-substitutedaryl-8-substitutedarylidene-2-imino-6-methyl-5,6-dihydro- 4H, 7H (3,1) benzothiazines. The structure of synthesized compounds were characterized by their UV, IR, 1H NMR and Mass spectral data as well as elemental analyses and newly synthesized final compounds were evaluated for their antimicrobial&anticonvulsant activity by PTZ induced method, using ciprofloxacin, fluconazole and diazepam as standard drugs.

Keywords

Chalcones, Thiazine, Antimicrobial Activity, Anticonvulsant Activity.
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  • Synthesis, Characterization and Biological Evaluation of Some Novel Substituted 1, 3-Thaizine Derivatives

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Authors

Srinivasa Murthy Muppavarapu
Department of Pharmaceutical Chemistry, Vignan Institute of Pharmaceutical Sciences, Near Ramoji Film City, Deshmukhi, Nalgonda, Telangana-508284, India
Ravindar Bairam
Department of Pharmaceutical Chemistry, Vignan Institute of Pharmaceutical Sciences, Near Ramoji Film City, Deshmukhi, Nalgonda, Telangana-508284, India

Abstract


Thiazine derivatives are an important class of heterocyclic compounds and reported to possess a wide spectrum of biological properties. Thiazines exerted important anticonvulsant activity in models of generalized seizure which were well documented in the literature and therefore new thiazines were synthesized with an aim to get potent anticonvulsant agents. 4-methyl Cyclohexanone on Claisen-Schmidt condensation with various aromatic aldehydes in presence of dilute sodium hydroxide afforded the corresponding 2,6-disubstitutedarylidene cyclohexanones. Further these compounds were subjected to cyclocondensation with thiourea, catalyzed by aqueous potassium hydroxide to form 4-substitutedaryl-8-substitutedarylidene-2-imino-6-methyl-5,6-dihydro- 4H, 7H (3,1) benzothiazines. The structure of synthesized compounds were characterized by their UV, IR, 1H NMR and Mass spectral data as well as elemental analyses and newly synthesized final compounds were evaluated for their antimicrobial&anticonvulsant activity by PTZ induced method, using ciprofloxacin, fluconazole and diazepam as standard drugs.

Keywords


Chalcones, Thiazine, Antimicrobial Activity, Anticonvulsant Activity.