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Updated: Oct 2, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Synthesis and antibacterial activity of some novel N-substituted piperazinyl-quinolones
A Foroumadi1, A Davood, M Mirzaei
1Department of Medicinal Chemistry, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran.
Abstract:
A series of N-substituted-piperazinyl-quinolones were synthesized and evaluated for in vitro antibacterial activity. Compounds with a 2-(2,4-dichlorophenyl)-2-oxoethyl group attached to the piperazine ring (5a-c) had similar antibacterial activity to the reference drugs, ciprofloxacin, norfloxacin and enoxacin against both Gram-positive and Gram-negative bacteria. The oximes 6a-c and 6g-i were almost less active than corresponding ketones against the tested microorganisms, however the 2,4-difluorophenyl analogues (6g-i) were more active than 2,4-dichlorophenyl derivatives (6a-c). If the hydrogen of oxime is replaced with a benzyl group (6d-f & 6j-l), in-vitro antibacterial activity was decreased against both Gram-positive and Gram-negative bacteria. Generally ciprofloxacin derivatives were more active than norfloxacin and enoxacin derivatives.
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