Medicinal Chemistry

Dimitra Hadjipavlou-Litina
Aristotle University of Thessaloniki
Thessaloniki
Greece

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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, Sushant K. Shrivastava.

Graphical Abstract:


Abstract:

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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Article Details

VOLUME: 10
ISSUE: 8
Year: 2014
Page: [800 - 809]
Pages: 10
DOI: 10.2174/1573406410666140402152044
Price: $58