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Medicinal Chemistry
ISSN (Print): 1573-4064
ISSN (Online): 1875-6638
Epub Full Text Article
DOI: 10.2174/1573406410666140402152044      Price:  $95









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

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Author(s): Nirupam Das, Anupam G. Banerjee and Sushant K. Shrivastava
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
Affiliation:
Department of Pharmaceutics, Indian Institute of Technology (BHU), Varanasi–221 005, India