scholarly journals Antibacterial Activity of Chloramphenicol-Related Compounds toward a Chloramphenicol-Resistant Strains ofStaphylococcus aureus

1972 ◽  
Vol 16 (6) ◽  
pp. 461-467 ◽  
Author(s):  
Megumi Kono ◽  
Koji O'Hara ◽  
Masatoshi Nagawa ◽  
Susumu Mitsuhashi
2000 ◽  
Vol 44 (4) ◽  
pp. 848-852 ◽  
Author(s):  
C. M. Kunin ◽  
W. Y. Ellis

ABSTRACT Mefloquine was found to have bactericidal activity against methicillin- and fluoroquinolone-susceptible and -resistant strains ofStaphylococcus aureus and Staphylococcus epidermidis and gentamicin- and vancomycin-resistant strains ofEnterococcus faecalis and Enterococcus faecium. The MICs were 16 μg/ml, and the minimal bactericidal concentrations (MBCs) were 16 to 32 μg/ml. These concentrations cannot be achieved in serum. Mefloquine was active at a more achievable concentration against penicillin-susceptible and -resistant Streptococcus pneumoniae, with MICs of 0.2 to 1.5 μg/ml. Mefloquine was not active against gram-negative bacteria and yeasts. In an attempt to find more active derivatives, 400 mefloquine-related compounds were selected from the chemical inventory of The Walter Reed Army Institute of Research. We identified a series of compounds containing a piperidine methanol group attached to pyridine, quinoline, and benzylquinoline ring systems. These had activities similar to that of mefloquine against S. pneumoniae but were far more active against other gram-positive bacteria (MICs for staphylococci, 0.8 to 6.3 μg/ml). They had activities similar to that of amphotericin B againstCandida spp. and Cryptococcus neoformans. Combinations of the compounds with gentamicin and vancomycin were additive against staphylococci and pneumococci. The MIC and MBC of gentamicin were decreased by four- to eightfold when this drug was combined with limiting dilutions of the compounds. There was no antagonism with other antimicrobial drugs. The compounds were rapidly bactericidal. They appear to act by disrupting cell membranes. Combinations of the compounds with aminoglycoside antibiotics may have potential for therapeutic use.


2018 ◽  
Vol 6 (6) ◽  
pp. 1-6
Author(s):  
Yao KANGA ◽  
CAMARA Djeneb ◽  
KOUASSI Kouadio Aubin ◽  
ZIRIHI Guédé Noël

The emergence of multi-drug resistant strains and limitations of present antimicrobial drugs have led to continuous search for natural products as curative agents for Anti-methicillin resistantinfections. The aim of this study was to evaluate antibacterial activity of an ethanolic extract from Albizia lebbeckstem bark against Anti-methicillin resistant. Methods and Results : The methods of dissemination swab on muller-hinton agar and double dilution were used to evaluate the antibacterial activity of 70 % ethanolic extract of stem bark of Albizia lebbeck.All multi-resistant strains of Staphylococcus aureus and the reference strain (ATCC 25923) were sensitive to 70 % ethanolic extract of the stem bark of Albizia lebbeck. The MBCvary from 0,49 mg/mL to 2mg/mL. Also, the phytochemical screening of this extract revealed the presence of  Polyphenols, Gallic tannins, Catechin tanninsand Flavonoids. These findings confirm that an 70 % ethanolic extract from Albizia lebbeck stem bark inhibited growth of Anti-methicillin resistant at low concentration and could be utilised as an alternative Anti-methicillin resistantagent.


2012 ◽  
Vol 4 (1) ◽  
pp. 13 ◽  
Author(s):  
Tatiane S. Coelho ◽  
Jessica B. Cantos ◽  
Marcelle L.F. Bispo ◽  
Raoni S.B. Gonçalves ◽  
Camilo H.S. Lima ◽  
...  

A series of twenty-three <em>N-acylhydrazones</em> derived from isoniazid (INH 1-23) have been evaluated for their <em>in vitro</em> antibacterial activity against INH- susceptible strain of <em>M. tuberculosis</em> (RG500) and three INH-resistant clinical isolates (RG102, RG103 and RG113). In general, derivatives 4, 14, 15 and 16 (MIC=1.92, 1.96, 1.96 and 1.86 mM, respectively) showed relevant activities against RG500 strain, while the derivative 13 (MIC=0.98 mM) was more active than INH (MIC=1.14 mM). However, these derivatives were inactive against RGH102, which displays a mutation in the coding region of <em>inhA</em>. These results suggest that the activities of these compounds depend on the inhibition of this enzyme. However, the possibility of other mechanisms of action cannot be excluded, since compounds 2, 4, 6, 7, 12-17, 19, 21 and 23 showed good activities against <em>katG</em>-resistant strain RGH103, being more than 10-fold more active than INH.


2020 ◽  
Vol 49 (21) ◽  
pp. 6980-6988
Author(s):  
Máté Kozsup ◽  
Donal M. Keogan ◽  
Deirdre Fitzgerald-Hughes ◽  
Éva A. Enyedy ◽  
Brendan Twamley ◽  
...  

Bidentate (O,O′) N-formylhydroxylamine chelation of Co(iii) centres and notable antibacterial activity of a Co(iii) peptide deformylase inhibitor complex against sensitive and resistant strains of S. aureus.


2020 ◽  
Vol 16 ◽  
pp. 117693432093626
Author(s):  
Iván Darío Ocampo-Ibáñez ◽  
Yamil Liscano ◽  
Sandra Patricia Rivera-Sánchez ◽  
José Oñate-Garzón ◽  
Ashley Dayan Lugo-Guevara ◽  
...  

Infections caused by multidrug-resistant (MDR) Pseudomonas aeruginosa and Klebsiella pneumoniae are a serious worldwide public health concern due to the ineffectiveness of empirical antibiotic therapy. Therefore, research and the development of new antibiotic alternatives are urgently needed to control these bacteria. The use of cationic antimicrobial peptides (CAMPs) is a promising candidate alternative therapeutic strategy to antibiotics because they exhibit antibacterial activity against both antibiotic susceptible and MDR strains. In this study, we aimed to investigate the in vitro antibacterial effect of a short synthetic CAMP derived from the ΔM2 analog of Cec D-like (CAMP-CecD) against clinical isolates of K pneumoniae (n = 30) and P aeruginosa (n = 30), as well as its hemolytic activity. Minimal inhibitory concentrations (MICs) and minimal bactericidal concentrations (MBCs) of CAMP-CecD against wild-type and MDR strains were determined by the broth microdilution test. In addition, an in silico molecular dynamic simulation was performed to predict the interaction between CAMP-CecD and membrane models of K pneumoniae and P aeruginosa. The results revealed a bactericidal effect of CAMP-CecD against both wild-type and resistant strains, but MDR P aeruginosa showed higher susceptibility to this peptide with MIC values between 32 and >256 μg/mL. CAMP-CecD showed higher stability in the P aeruginosa membrane model compared with the K pneumoniae model due to the greater number of noncovalent interactions with phospholipid 1-Palmitoyl-2-oleyl-sn-glycero-3-(phospho-rac-(1-glycerol)) (POPG). This may be related to the boosted effectiveness of the peptide against P aeruginosa clinical isolates. Given the antibacterial activity of CAMP-CecD against wild-type and MDR clinical isolates of P aeruginosa and K pneumoniae and its nonhemolytic effects on human erythrocytes, CAMP-CecD may be a promising alternative to conventional antibiotics.


2005 ◽  
Vol 60 (2) ◽  
pp. 183-188 ◽  
Author(s):  
R. P. Maskey ◽  
H. Lessmann ◽  
S. Fotso ◽  
I. Grün-Wollny ◽  
H. Lackner ◽  
...  

From the Streptomyces spp. 815 and GW4184, four new 4-juglon-2-ylbutyric acid derivatives, the juglomycins G - J (3a, 4a, 4c, 5c), have been isolated and characterised. The structures were derived from the 1D and 2D NMR data and mass spectra and confirmed by comparison with structurally related compounds. The absolute configuration was deduced from the CD spectra. The new natural products exhibited weak antibacterial activity similar to juglomycin A (5a).


Pathogens ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 542 ◽  
Author(s):  
John J. Mackrill ◽  
Roberta A. Kehoe ◽  
Limian Zheng ◽  
Mary L. McKee ◽  
Elaine C. O’Sullivan ◽  
...  

The pathogen Phytophthora infestans is responsible for catastrophic crop damage on a global scale which totals billions of euros annually. The discovery of new inhibitors of this organism is of paramount agricultural importance and of critical relevance to food security. Current strategies for crop treatment are inadequate with the emergence of resistant strains and problematic toxicity. Natural products such as cinnamaldehyde have been reported to have fungicidal properties and are the seed for many new discovery research programmes. We report a probe of the cinnamaldehyde framework to investigate the aldehyde subunit and its role in a subset of aromatic aldehydes in order to identify new lead compounds to act against P. infestans. An ellipticine derivative which incorporates an aldehyde (9-formyl-6-methyl ellipticine, 34) has been identified with exceptional activity versus P. infestans with limited toxicity and potential for use as a fungicide.


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