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Thiadiazole Derivatives as Potential Anticonvulsant Agents

  • Mullick, Pooja (Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University) Hamdard Nagar) ;
  • Khan, Suroor A. (Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University) Hamdard Nagar) ;
  • Verma, Surajpal (Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University) Hamdard Nagar) ;
  • Alam, Ozair (Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University) Hamdard Nagar)
  • Received : 2010.08.30
  • Accepted : 2010.12.20
  • Published : 2011.03.20

Abstract

A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR, $^1H$ NMR, $^{13}C$ NMR and mass spectral data confirmed the structure of the synthesized compounds. The derivatives of these moieties were evaluated for anticonvulsant activity by MES model and neurotoxicity by rotarod method. The synthesized compounds showed good potential for anticonvulsant activity besides this, the compounds also showed neurotoxic effect. It was observed that compounds with $OCH_3$ at 3, 4 position of phenyl ring [5(a-l)] showed less protection against convulsions as compared to compounds having unsubstituted phenyl ring [4(a-l)].

Keywords

References

  1. Pandeya, S. N.; Raja, A. S.; Stables, J. P. J. Pharm. PharmaceutSci. 2002, 5(3), 266.
  2. Krall, R. L.; Penry, J.K.;White, B.G.;Kupferberg,H. J.; Swinyard,E. A. Epilepsia 1978, 19, 409. https://doi.org/10.1111/j.1528-1157.1978.tb04507.x
  3. White, H. S.; Johnson, M.;Wolf, H. H.; Kupferberg, H. J. Ital. J.Sci. 1995, 16, 73. https://doi.org/10.1007/BF02229077
  4. Dunham, M. S.; Miya, T. A. J. Am. Pharmac. Assoc. Sci. Edit.1957, 46, 208.
  5. Shafiee, A.; Naimi, E.; Mansobi, P.; Foroumadi, A.; Shekari,M.J. Het. Chem. 1995, 32, 1235. https://doi.org/10.1002/jhet.5570320424
  6. Altıntaş, H.; Ateş, O.; Kocabalkanli, A.; Birteksoz, S.; Otuk, G.Ind. J. Chem. 2005, 44B, 585.

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