Acta Pharm. 59 (2009) 441-451

full paper

Original research paper

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

NADEEM SIDDIQUI, ARPANA RANA, SUROOR A. KHAN, S. EHTAISHAMUL HAQUE, M. FAIZ ARSHAD, SHARIQUE AHMED and WAQUAR AHSAN

nadeems_03@yahoo.co.in, nadeems_03@rediffmail.com

¹Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi-110062, India

²Department of Pharmacology, Faculty of Pharmacy, Hamdard University, New Delhi-110062, India

³Department of Biochemistry, Faculty of Medicine, 7^th October University, Misurata, Libya

Accepted July 27, 2009

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 the seizure spread. Compounds 5b and 5c showed complete protection against MES induced seizures.

Keywords: benzothiazole, thiadiazole, anticonvulsant, neurotoxicity, hepatotoxicity