Synthesis of New 2,5-Disubstituted-1,3,4-Thiadiazole Derivatives and Their in vivo Anticonvulsant Activity

K. P. Harish^{a, #}, K. N. Mohana^a, and L. Mallesha^b

^#Phone: +91-9845677501; e-mail: dhruvaharishp@gmail.com

^aDepartment of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, India;
^bPG Department of Chemistry, JSS College of Arts, Commerce and Science, Ooty Road, Mysore-25, India

Received May 17, 2013; in final form July 3, 2013

A series of 2,5-disubstituted-1,3,4-thiadiazole derivatives were synthesized by the reaction of 3-(2-cyanopropan-2-yl)-N-(5-(piperazine-1-yl)-1,3,4-thiadiazol-2-yl)benzamide with various sulfonyl chlorides and evaluated for their anticonvulsant activity in MES test. Rotorod method was employed to determine the neurotoxicity. The purity of the compounds is confirmed on the basis of their elemental analysis. The structures of all the new compounds are established on the basis of ¹H NMR and mass spectral data. Out of fifteen compounds, three were found to be potent anticolvunstants. The same compounds showed no neurotoxicity at the maximum dose administered (100 mg/kg).

Keywords: 1,3,4-thiadiazole, anticonvulsant, neurotoxicity

Биоорг. химия 2014, 40 (1): 108-116