Design, Synthesis and Biological Activity of Some 4, 5-Disubstituted-2, 4- Dihydro-3H-1, 2, 4- Triazole-3-Thione Derivatives

Author(s): Krishan Kumar Verma*, Umesh Kumar Singh, Jainendra Jain.

Journal Name: Central Nervous System Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Central Nervous System Agents)

Volume 19 , Issue 3 , 2019

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Abstract:

Background: In the present study, 4, 5-disubstituted triazol-3-thione derivatives were synthesized and evaluated for anticonvulsant activity along with neurotoxicity determination.

Materials and Methods: The synthesized compounds were characterized using FTIR, 1H-NMR and MS. The anticonvulsant activity was assessed by Maximal Electroshock (MES) test and subcutaneous Pentylenetetrazole (scPTZ) tests and neurotoxicity was assessed by rotarod test. Docking was also performed to study the interactions of compounds with LYS329 residue of gamma amino butyric acid aminotransferase (GABA-AT) using Autodock 4.2 software.

Results: The compounds 7a and 9a with significant pharmacological activity were also found to interact with LYS329 residue of GABA-AT by H-bond with a docking score of -5.92 kcal/mol (Ki = 41.99 μM) and -5.87 kcal/mol (Ki = 49.83 μM) respectively.

Conclusion: Most of the compounds were found to be active in MES test but only seven showed protection in scPTZ test.

Keywords: Triazol-3-thiones, anticonvulsant, scPTZ, MES, docking, GABA-AT.

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Article Details

VOLUME: 19
ISSUE: 3
Year: 2019
Page: [197 - 205]
Pages: 9
DOI: 10.2174/1871524919666190722144424

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