Letters in Drug Design & Discovery

Atta-ur-Rahman  , FRS
Honorary Life Fellow
Kings College
University of Cambridge
Email: lddd@benthamscience.org


Development of 1, 3 Benzothiazol-2-yl Hydrazine Derivatives Containing Semicarbazone and Thioamide Pharmacophore as Anticonvulsants

Author(s): Ruhi Ali and Nadeem Siddiqui

Affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi-110062, India.

Graphical Abstract:


Newer N-(6-substitutedbenzo[d]thiazol-2-yl)-2-((substitutedcarbamothioyl)hydrazinecarboxamides were synthesized having semicarbazone and thioamide as two hydrogen bonding domains attached between proximal and distal aryl rings with a view to explore prospective anticonvulsant candidates. For preliminary screening of synthesized compounds, two convulsant tests i.e. Maximal electroshock (MES) and subcutaneous Pentylenetetrazole (scPTZ) tests were performed. Rotarod test was performed to determine any possible neurotoxicity in the synthesized compounds. The result of anticonvulsant screening established the significant ability of compounds, 3i, 3j and 3m, to suppress the convulsions generated by electrical seizures and scPTZ induced seizures as compared to standard drugs phenytoin (PHY) and carbamazepine (CBZ). Molecular properties and Pharmacokinetic parameters of the titled compounds were also determined using Lipinski’s rule of five. The promising results encourage future investigation on the rational modification of this nucleus for development of better compounds.

Keywords: Anticonvulsant, benzothiazole, semicarbazone, thioamide, pharmacokinetic, neurotoxicity.

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Article Details

Page: [1214 - 1224]
Pages: 11
DOI: 10.2174/1570180811666140627004353