Title: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
VOLUME: 10 ISSUE: 8
Author(s):Nirupam Das, Anupam G. Banerjee and Sushant K. Shrivastava
Affiliation:Department of Pharmaceutics, Indian Institute of Technology (BHU), Varanasi-221 005, India.
Keywords:Anticonvulsant activity, AMPA induced seizure, hepatotoxicity, neurotoxicity, quinazolin-4(3H)-ones, synthesis.
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.
