DOI QR코드

DOI QR Code

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)].

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.

Cited by

  1. ChemInform Abstract: Thiadiazole Derivatives as Potential Anticonvulsant Agents. vol.42, pp.29, 2011, https://doi.org/10.1002/chin.201129129
  2. Synthetic Methods, Chemistry, and the Anticonvulsant Activity of Thiadiazoles vol.2013, pp.2090-2077, 2013, https://doi.org/10.1155/2013/348948
  3. Recent Advances in the Chemistry and Synthetic Uses of Amino-1,3,4-thiadiazoles vol.51, pp.6, 2014, https://doi.org/10.1002/jhet.1872
  4. Molecular sieves promoted, ultrasound-mediated synthesis, biological evaluation and docking study of 3-(5-substituted-1,3,4-thiadiazol-2-ylimino)indolin-2-ones as a potential anticonvulsant agents vol.24, pp.12, 2015, https://doi.org/10.1007/s00044-015-1458-x
  5. 1,3,4-Thiadiazol-2-amine Derivatives as Urotensin-II Receptor (UT) Antagonists vol.36, pp.10, 2015, https://doi.org/10.1002/bkcs.10475
  6. A facile access and evaluation of some novel thiazole and 1,3,4-thiadiazole derivatives incorporating thiazole moiety as potent anticancer agents vol.11, pp.1, 2017, https://doi.org/10.1186/s13065-017-0335-8