Design, Synthesis and Pharmacological Evaluation of N3 Aryl/heteroaryl Substituted 2–((Benzyloxy and Phenylthio) Methyl) 6,7–Dimethoxyquinazolin–4(3H)–Ones as Potential Anticonvulsant Agents

ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)


Volume 10, 8 Issues, 2014


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Medicinal Chemistry

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Design, Synthesis and Pharmacological Evaluation of N3 Aryl/heteroaryl Substituted 2–((Benzyloxy and Phenylthio) Methyl) 6,7–Dimethoxyquinazolin–4(3H)–Ones as Potential Anticonvulsant Agents

Author(s): Nirupam Das, Anupam G. Banerjee and Sushant K. Shrivastava

Affiliation: Department of Pharmaceutics, Indian Institute of Technology (BHU), Varanasi–221 005, India

Abstract

Novel N3 aryl/heteroaryl substituted 2–((benzyloxy and phenylthio) methyl) 6,7–dimethoxyquinazolin–4(3H)–ones (8a–8l) have been synthesized and assessed for anticonvulsant activity using various model of epilepsy such as maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ) and intracerebroventricular AMPA (α–amino–3–hydroxy–5–methyl–4–isoxazolepropionic acid)–induced seizures in mice. The acute neurotoxicity was determined using the rotarod test and hepatotoxicity was assessed by estimating the aspartate aminotransferase (AST) and alanine aminotransferase (ALT) enzyme activity along with histopathological study. Compound 8f displayed encouraging activity profile among all the compounds in the series based on overall magnitude of activity and minimal neurotoxicity

Keywords: Anticonvulsant activity, AMPA induced seizure, hepatotoxicity, neurotoxicity, quinazolin-4(3H)-ones, synthesis

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Article Details

Volume: 10
First Page: 1
Last Page: 10
Page Count: 10
DOI: 10.2174/1573406410666140402152044
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