SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SOME NOVEL SCHIFF BASE 1, 3-THIAZINE DERIVATIVES
Abstract
Although many active anticonvulsant drugs have since been developed, a disturbing co-occurrence with the use of present drugs as single agent has developed drug resistance. This has made use to investigate for new thiazine derivatives for finding more effective anticonvulsant agents. The present investigation, was designed a new series of 2-amino-4-phenyl-6H-1, 3-thiazine indolin-2-one derivatives (3a-j) were synthesized from 1,3-thiazine derivatives. In the beginning acetophenone which underwent Claisen-Schmidt condensation, was dissolved in ethanol and various substituted aromatic aldehydes were added in the presence basic media to afford chalcones (1a-j). Further these various chalcones were subjected to cyclocondensation with thiourea, in ethyl alcohol, catalyzed by aqueous potassium hydroxide to afford 1, 3-thiazine derivatives (2a-j). Now these 1,3-thiazine derivatives were refluxed with substituted isatin catalyzed by glacial acetic acid in ethanol to afford 2-amino-4-phenyl-6H-1,3-thiazine indolin-2-one derivatives (3a-j). The structures of the newly synthesized compounds have been characterized by their infrared spectroscopy, proton nuclear magnetic resonance, 13Carbon nuclear magnetic resonance, mass spectral data and elemental analysis. These newly synthesized compounds were screened for their anticonvulsant activity. Anticonvulsant activity has been done by Maximal electroshock (MES) method and pentylenetetrazole (PTZ) induced method. These compounds were subjected to molecular property prediction, drug-likeness, lipophilicity and solubility parameters determination using Molinspiration, Osiris program was used for prediction of the toxicity.
Keywords: Claisen-Schmidt; 1,3-Thiazines; Schiff Base; Anticonvulsant activity
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How to cite this article:
Ravindar Bairam, and Srinivasa Murthy Muppavarap;, Synthesis, characterization and biological evaluation of some novel schiff base 1, 3-thiazine derivatives, Panacea Journal of Pharmacy and Pharmaceutical Sciences 2018:7(1); 719-734.
