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Medicinal Chemistry


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

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

Volume 10, Issue 8, 2014

Page: [800 - 809] Pages: 10

DOI: 10.2174/1573406410666140402152044

Price: $65


Novel N3 aryl/heteroaryl substituted 2-((benzyloxy and phenylthio) methyl) 6,7-dimethoxyquinazolin-4(3H)- ones (8a-8l) were synthesized and evaluated for their anticonvulsant activity using various models 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 rotarod test has been used to determine the acute neurotoxicity. Further, the serum enzymatic activities of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) were assessed along with histopathological examination of liver. Among all the derivatives, compound 8f displayed significant activity profile based on the overall magnitude of activity and minimum neurotoxicity.

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

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