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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Research Article

Synthesis and Some Reactions of 1-aryl-4-acetyl-5-methyl-1,2,3-triazole Derivatives with Anticonvulsant Activity

Author(s): Ekhlass M. Nassar, Fathy M. Abdelrazek, Rezk R. Ayyad and Ahmed F. El-Farargy

Volume 16, Issue 11, 2016

Page: [926 - 936] Pages: 11

DOI: 10.2174/1389557516666160118105505

Price: $65

Abstract

The triazoles 3a-d underwent condensation reactions with 4-(piperidin-1-yl)-benzaldehyde to afford the chalcones 5a-d. Chalcone derivatives 5a-d were reacted with 2,3-diaminomaleonitrile, thiourea and hydrazine hydrate to afford the novel diazepine-dicarbonitrile derivatives 7a-d, the pyrimidine-2-thiol derivatives 9a-d and hydrazino-pyrimidines 10a-d respectively. Structures of the prepared compounds were elucidated by physical and spectral data like FT-IR, 1H NMR, 13C NMR, and mass spectroscopy. Some of the synthesized compounds were screened for their anticonvulsant activity and SAR.

Keywords: Anticonvulsant activity, chalcones, diazepines, hydrazino-pyrimidines, pyrimidine-thioles, 1, 2, 3-triazoles, ultrasonication.

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