DOI: 10.21276/ajptr
Mon, 20 May 2019

Synthesis and Antimicrobial Evaluation of some novel 2, 3, 7-Trisubstituted Quinazolinones derivatives


Rajendra S. Dave*1, Rajendra J. Odedara1, Rushit I. Kalaria2, Jatin J. Upadhyay2.

1.Department of Chemistry, Smt. M. G. Panchal Sci. College, Pilvai, Gujarat, India.

2.MVM Science and Home Sci. College, Saurastra University, Rajkot, Gujarat, India.



Reaction of 4-chloro anthranilic acid 1 with chloroacetyl chloride followed by 4-fluoro aniline provides 7-chloro-2-(chloromethyl)-3-(4-fluorophenyl) quinazolin-4(3H)-one 3, which on treatment with 2-chloro benzimidazole in the presence of potassium carbonate yielded 7-chloro-2-(2-chloro-benzoimidazol-1-ylmethyl)-3-(4-fluorophenyl)-3H-quinazolin-4-one 4. The latter on reaction with nitrogen nucleophiles in acetone containing K2CO3 and catalytic amount of KI gave novel 7-Chloro-3-(4-fluoro phenyl)-2-((substituted amino -1H-benz[d]imidazol-1-yl)methyl) quinazolin-4(3H)-one derivatives 5a-h. Furthermore all the compounds were also tested against Gram negative, Gram positive bacteria and fungi. Among the compound tested in this study, compounds 2-(2-pyrrolidin-1-yl-benzimidazol-1-ylmethyl)-3H-quinazolin-4-one (5b) and 2-(2-piperidin-1-yl-benzimidazol-1-ylmethyl)-3H-quinazolin-4-one (5c) found more potent against S. aureus and E. coli compare to reference standard ampicillin.

Keywords: Quinazolin-4(3H)-one, nucleophilic substitution, antibacterial activity, antifungal activity.

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