Open AccessSYNTHESIS AND EVALUATION OF ANTIMICROBIAL ACTIVITY OF QUINAZOLINONE DERIVATIVES
Author(s) -
Pratap Y. Pawar,
M Waghmare Sweeti
Publication year - 2020
Publication title -
international journal of current pharmaceutical research
Language(s) - English
Resource type - Journals
ISSN - 0975-7066
DOI - 10.22159/ijcpr.2020v12i3.38318
Subject(s) - quinazolinone , chemistry , acetamide , chloroacetyl chloride , antimicrobial , organic chemistry , hydrazine (antidepressant) , chloride , medicinal chemistry , biochemistry
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.