4.7 Article

Quinazolino-benzothiazoles: Fused pharmacophores as anticonvulsant agents

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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 53, 期 -, 页码 107-113

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ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.03.045

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Synthesis quinazolino-benzothiazoles; MES; PTZ-induced seizure; Neurotoxicity; Hepatotoxicity

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A series of 6-bromo-2-ethyl-3-(substitutedbenzo[d]thiazol-2-yl)quinazolin-4(3H)-one 3 (a-j) were synthesized using appropriate synthetic route and evaluated experimentally by the Maximal Electro Shock (MES) and the PTZ-induced seizure methods. Among the tested compounds, 3-(benzo[d]thiazol-2-yl)-6-bromo-2-ethylquinazolin-4(3H)-one (3a) has shown significant activity against tonic seizure by the MES model and 6-bromo-2-ethyl-3-(6-methoxybenzo[d]thiazol-2-yl)quinazolin-4(3H)-one (3h) against clonic seizure by PTZ-induced seizure model. Not one of the selected compounds demonstrated any sign of neurotoxicity and hepatotoxicity. (C) 2012 Elsevier Masson SAS. All rights reserved.

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