Synthesis and preliminary screening of benzothiazol-2-yl thiadiazole derivatives for anticonvulsant activity

Acta Pharm. 2009 Dec;59(4):441-51. doi: 10.2478/v10007-009-0031-x.

Abstract

Various N-(5-chloro-6-substituted-benzothiazol-2-yl)-N'-(substituted phenyl)-[1,3,4]thiadiazole-2,5-diamines (5a-t) were designed and synthesized starting from substituted acetophenones. Structures of all the compounds were confirmed on the basis of spectral and elemental analyses. All the newly synthesized compounds were screened for their anticonvulsant activity and were compared with the standard drug phenytoin sodium. Interestingly, all the compounds showed protections against seizures in the range 50-100% indicative of the promising nature of the compounds against seizure spread. Compounds 5b and 5c showed complete protection against MES induced seizures.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetophenones
  • Animals
  • Anticonvulsants / chemical synthesis
  • Anticonvulsants / chemistry*
  • Anticonvulsants / pharmacology*
  • Drug Evaluation, Preclinical
  • Mice
  • Seizures / drug therapy
  • Thiadiazoles / chemical synthesis
  • Thiadiazoles / chemistry*
  • Thiadiazoles / pharmacology*

Substances

  • Acetophenones
  • Anticonvulsants
  • Thiadiazoles
  • acetophenone