Quinazolin-4-ones with 2, 3-disubstitution is reported to possess significant analgesic, anti-inflammatory and anticonvulsant activities. We have developed an efficient method for the synthesis of 3-substituted-2-methylquinazolin-4-one by the condensation reaction of Anthranilic acid, acetic anhydride with various amines. The synthesized compounds were evaluated for anxiolytic activity by Elevated plus Maze Test and Light and Dark Test. It is observed that the aliphatic and aromatic substitution at 3-position of 2-methylquinazolin-4-one gives potent anxiolytic activity. In particular, ENA showed highest anxiolytic activity in Elevated plus Maze Test and EMQ and AMQ showed highest anxiolytic activity in Light and dark test model
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