In Vitro Bactericidal Activity of 4- and 5-Chloro-2-hydroxy-N-[1-oxo-1-(phenylamino)alkan-2-yl]benzamides against MRSA
A series of nine substituted 2-hydroxy-N-[1-oxo-1-(phenylamino)alkan-2-yl]benzamides was assessed as prospective bactericidal agents against three clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) and S. aureus ATCC 29213 as the reference and quality control strain. The minimum...
Main Authors: | , , , , , , |
---|---|
Format: | Article |
Language: | English |
Published: |
Hindawi Limited
2015-01-01
|
Series: | BioMed Research International |
Online Access: | http://dx.doi.org/10.1155/2015/349534 |
id |
doaj-43497168c17b4a0bbc3bff4aecbea1c2 |
---|---|
record_format |
Article |
spelling |
doaj-43497168c17b4a0bbc3bff4aecbea1c22020-11-24T21:47:51ZengHindawi LimitedBioMed Research International2314-61332314-61412015-01-01201510.1155/2015/349534349534In Vitro Bactericidal Activity of 4- and 5-Chloro-2-hydroxy-N-[1-oxo-1-(phenylamino)alkan-2-yl]benzamides against MRSAIveta Zadrazilova0Sarka Pospisilova1Karel Pauk2Ales Imramovsky3Jarmila Vinsova4Alois Cizek5Josef Jampilek6Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackeho 1/3, 612 42 Brno, Czech RepublicDepartment of Infectious Diseases and Microbiology, Faculty of Veterinary Medicine, University of Veterinary and Pharmaceutical Sciences Brno, Palackeho 1/3, 612 42 Brno, Czech RepublicInstitute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech RepublicInstitute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech RepublicDepartment of Inorganic and Organic Chemistry, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech RepublicDepartment of Infectious Diseases and Microbiology, Faculty of Veterinary Medicine, University of Veterinary and Pharmaceutical Sciences Brno, Palackeho 1/3, 612 42 Brno, Czech RepublicDepartment of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackeho 1/3, 612 42 Brno, Czech RepublicA series of nine substituted 2-hydroxy-N-[1-oxo-1-(phenylamino)alkan-2-yl]benzamides was assessed as prospective bactericidal agents against three clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) and S. aureus ATCC 29213 as the reference and quality control strain. The minimum bactericidal concentration was determined by subculturing aliquots from MIC determination onto substance-free agar plates. The bactericidal kinetics of compounds 5-chloro-2-hydroxy-N-[(2S)-3-methyl-1-oxo-1-{[4-(trifluoromethyl)phenyl]amino}butan-2-yl]benzamide (1f), N-{(2S)-1-[(4-bromophenyl)amino]-3-methyl-1-oxobutan-2-yl}-4-chloro-2-hydroxybenzamide (1g), and 4-chloro-N-{(2S)-1-[(3,4-dichlorophenyl)amino]-3-methyl-1-oxobutan-2-yl}-2-hydroxybenzamide (1h) was established by time-kill assay with a final concentration of the compound equal to 1x, 2x, and 4x MIC; aliquots were removed at 0, 4, 6, 8, and 24 h time points. The most potent bactericidal agent was compound 1f exhibiting remarkable rapid concentration-dependent bactericidal effect even at 2x MIC at 4, 6, and 8 h (with a reduction in bacterial count ranging from 3.08 to 3.75 log10 CFU/mL) and at 4x MIC at 4, 6, 8, and 24 h (5.30 log10 CFU/mL reduction in bacterial count) after incubation against MRSA 63718. Reliable bactericidal effect against other strains was maintained at 4x MIC at 24 h.http://dx.doi.org/10.1155/2015/349534 |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Iveta Zadrazilova Sarka Pospisilova Karel Pauk Ales Imramovsky Jarmila Vinsova Alois Cizek Josef Jampilek |
spellingShingle |
Iveta Zadrazilova Sarka Pospisilova Karel Pauk Ales Imramovsky Jarmila Vinsova Alois Cizek Josef Jampilek In Vitro Bactericidal Activity of 4- and 5-Chloro-2-hydroxy-N-[1-oxo-1-(phenylamino)alkan-2-yl]benzamides against MRSA BioMed Research International |
author_facet |
Iveta Zadrazilova Sarka Pospisilova Karel Pauk Ales Imramovsky Jarmila Vinsova Alois Cizek Josef Jampilek |
author_sort |
Iveta Zadrazilova |
title |
In Vitro Bactericidal Activity of 4- and 5-Chloro-2-hydroxy-N-[1-oxo-1-(phenylamino)alkan-2-yl]benzamides against MRSA |
title_short |
In Vitro Bactericidal Activity of 4- and 5-Chloro-2-hydroxy-N-[1-oxo-1-(phenylamino)alkan-2-yl]benzamides against MRSA |
title_full |
In Vitro Bactericidal Activity of 4- and 5-Chloro-2-hydroxy-N-[1-oxo-1-(phenylamino)alkan-2-yl]benzamides against MRSA |
title_fullStr |
In Vitro Bactericidal Activity of 4- and 5-Chloro-2-hydroxy-N-[1-oxo-1-(phenylamino)alkan-2-yl]benzamides against MRSA |
title_full_unstemmed |
In Vitro Bactericidal Activity of 4- and 5-Chloro-2-hydroxy-N-[1-oxo-1-(phenylamino)alkan-2-yl]benzamides against MRSA |
title_sort |
in vitro bactericidal activity of 4- and 5-chloro-2-hydroxy-n-[1-oxo-1-(phenylamino)alkan-2-yl]benzamides against mrsa |
publisher |
Hindawi Limited |
series |
BioMed Research International |
issn |
2314-6133 2314-6141 |
publishDate |
2015-01-01 |
description |
A series of nine substituted 2-hydroxy-N-[1-oxo-1-(phenylamino)alkan-2-yl]benzamides was assessed as prospective bactericidal agents against three clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) and S. aureus ATCC 29213 as the reference and quality control strain. The minimum bactericidal concentration was determined by subculturing aliquots from MIC determination onto substance-free agar plates. The bactericidal kinetics of compounds 5-chloro-2-hydroxy-N-[(2S)-3-methyl-1-oxo-1-{[4-(trifluoromethyl)phenyl]amino}butan-2-yl]benzamide (1f), N-{(2S)-1-[(4-bromophenyl)amino]-3-methyl-1-oxobutan-2-yl}-4-chloro-2-hydroxybenzamide (1g), and 4-chloro-N-{(2S)-1-[(3,4-dichlorophenyl)amino]-3-methyl-1-oxobutan-2-yl}-2-hydroxybenzamide (1h) was established by time-kill assay with a final concentration of the compound equal to 1x, 2x, and 4x MIC; aliquots were removed at 0, 4, 6, 8, and 24 h time points. The most potent bactericidal agent was compound 1f exhibiting remarkable rapid concentration-dependent bactericidal effect even at 2x MIC at 4, 6, and 8 h (with a reduction in bacterial count ranging from 3.08 to 3.75 log10 CFU/mL) and at 4x MIC at 4, 6, 8, and 24 h (5.30 log10 CFU/mL reduction in bacterial count) after incubation against MRSA 63718. Reliable bactericidal effect against other strains was maintained at 4x MIC at 24 h. |
url |
http://dx.doi.org/10.1155/2015/349534 |
work_keys_str_mv |
AT ivetazadrazilova invitrobactericidalactivityof4and5chloro2hydroxyn1oxo1phenylaminoalkan2ylbenzamidesagainstmrsa AT sarkapospisilova invitrobactericidalactivityof4and5chloro2hydroxyn1oxo1phenylaminoalkan2ylbenzamidesagainstmrsa AT karelpauk invitrobactericidalactivityof4and5chloro2hydroxyn1oxo1phenylaminoalkan2ylbenzamidesagainstmrsa AT alesimramovsky invitrobactericidalactivityof4and5chloro2hydroxyn1oxo1phenylaminoalkan2ylbenzamidesagainstmrsa AT jarmilavinsova invitrobactericidalactivityof4and5chloro2hydroxyn1oxo1phenylaminoalkan2ylbenzamidesagainstmrsa AT aloiscizek invitrobactericidalactivityof4and5chloro2hydroxyn1oxo1phenylaminoalkan2ylbenzamidesagainstmrsa AT josefjampilek invitrobactericidalactivityof4and5chloro2hydroxyn1oxo1phenylaminoalkan2ylbenzamidesagainstmrsa |
_version_ |
1725895163770830848 |