SYNTHESIS AND EVALUATION OF ANTIMICROBIAL ACTIVITY OF QUINAZOLINONE DERIVATIVES

Objective: The present study aims to synthesis and evaluation of antimicrobial activity of quinazolinone derivatives. Methods: Methyl anthranilate react with acetyl chloride in ethanol gives methyl-2 acetamido benzoate (1) which on reaction with hydrazine hydrate gives 3-amino-2 methyl 4-(3H)-quinazolinone.(2) The amino group of synthesized quinazolinone with substituted acid chloride which gives 3-Chloroacetyl amino-2-methyl-4-quinazolinone (3) which on condensation with various primary amines gives 2-(2-methyl-4-oxo-4H-quinazoline-3yl-amino)-N-substituted acetamide (4a-4j). Results: The reaction sequence involves microwave-induced preparation of methyl-2 acetamido benzoate (1) from reaction of Methyl anthranilate react with acetyl chloride in ethanol. Further reaction with hydrazine hydrate gives 3-amino-2 methyl 4-(3H)-quinazolinone. (2) The amino group of synthesized quinazolinone with substituted acid chloride which gives 3-Chloroacetyl amino-2-methyl-4-quinazolinone (3) which on condensation with various primary amines gives 2-(2-methyl-4-oxo-4H-quinazoline-3yl-amino)-N-substituted acetamide (4a-4j). Which were characterized by IR and 1HNMR spectral data. Conclusion: All the synthesized compounds were screened for antimicrobial activity by Broth dilution method. Most of the derivatives showed good antimicrobial activity against Gram-Positive and Gram-negative bacteria

BIOLOGICAL ACTIVITY OF QUINAZOLINONE DERIVATIVES: A REVIEW

The heterocyclic compounds have a great importance in medicinal chemistry. Quinazolinone is a heterocyclic chemical compound. A quinazolinone with a carbonyl group in the C4N2 ring. The two isomers are possible: 2-Quinazolinone and 4-Quinazolinone, with the 4-isomer being the more common. These compounds are of interest in medicinal chemistry. Quinazolinone derivatives were reported to possess analgesic and anti-inflammatory activity, Antibacterial, Diuretic, Antihypertensive, Anti-diabetics, Anticancer, Antitumor, Anti-fungal, Anti-malarial, Anti-protozoal agent and many other biological Action. This skeleton is an important pharmacophore considered as a privileged structure