Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12188/9561
Title: SYNTHESIS, PHYSICOCHEMICAL CHARACTERIZATION AND ANTIBACTERIAL ACTIVITY OF NOVEL (BENZOYLAMINO)METHYL DERIVATIVES OF QUINOLONES
Other Titles: СИНТЕЗА, ФИЗИЧКОХЕМИСКА КАРАКТЕРИЗАЦИЈА И АНТИБАКТЕРИСКА АКТИВНОСТ НА НОВИ (БЕНЗОИЛАМИНО)МЕТИЛНИ ДЕРИВАТИ НА ХИНОЛОНИ
Authors: P. Breznica-Selmani
K. Mladenovska 
G. Dräger
B. Mikhova
N. Panovski 
A. Kaftandzieva 
Z. Kavrakovski
A. Hoxha
N. Sheqerxhiu
M J Pavlova 
E. Popovski
Keywords: (benzoylamino)methyl
quinolones
structure
physicochemical properties
Issue Date: 2016
Publisher: MJCCA9 – 712
Journal: Macedonian Journal of Chemistry and Chemical Engineering
Abstract: Herein we report the synthesis of different derivatives of (fluoro)quinolones norfloxacin, ciprof-loxacin and pipemidic acid, by incorporating (benzoylamino)methyl on the free nitrogen of the pyperazi-nyl moiety. The compounds were structurally characterized by 1D and 2D NMR, FTIR and high-resolution mass spectroscopy. In addition, their physicochemical properties were a matter of interest to be correlated with their structure and antimicrobial activity in vitro. Their antimicrobial activities were screened against Gram-positive, Gram-negative bacteria and C. albicans. Higher distribution coefficients and consequently lower water solubility were determined for all synthesized compounds than the ones of the corresponding leading compounds. Inconsequential correlations between the lipophilicity of the compounds and MIC were observed, suggesting that passive diffusion is not the only mechanism for their penetration in-to bacterial cells. Further studies are needed to determine how substitutions in the (fluoro)quinolone moiety affect the primary target(s), substrate behavior in respect to bacterial transporters and overall bioavailability.
URI: http://hdl.handle.net/20.500.12188/9561
ISSN: ISSN 1857-5552
Appears in Collections:Faculty of Medicine: Journal Articles

Files in This Item:
File Description SizeFormat 
919-3634-1-PB.pdf1.29 MBAdobe PDFView/Open
Show full item record

Page view(s)

71
checked on Mar 28, 2024

Download(s)

17
checked on Mar 28, 2024

Google ScholarTM

Check


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.