Fluorocyclines. 1. 7-Fluoro-9-pyrrolidinoacetamido-6-demethyl-6-deoxytetracycline: A Potent, Broad Spectrum Antibacterial Agent

2012 ◽  
Vol 55 (2) ◽  
pp. 597-605 ◽  
Author(s):  
Xiao-Yi Xiao ◽  
Diana K. Hunt ◽  
Jingye Zhou ◽  
Roger B. Clark ◽  
Nick Dunwoody ◽  
...  
Author(s):  
Nidhi Sharma ◽  
Arti Singh ◽  
Ruchika Sharma ◽  
Anoop Kumar

Aim: The aim of the study was to find out the role of auranofin as a promising broad spectrum antibacterial agent. Methods: In-vitro assays (Percentage growth retardation, Bacterial growth kinetics, Biofilm formation assay) and In-silico study (Molegro virtual docker (MVD) version 6.0 and Molecular operating environment (MOE) version 2008.10 software). Results: The in vitro assays have shown that auranofin has good antibacterial activity against Gram positive and Gram negative bacterial strains. Further, auranofin has shown synergistic activity in combination with ampicillin against S. aureus and B. subtilis whereas in combination with neomycin has just shown additive effect against E. coli, P. aeruginosa and B. pumilus. In vivo results have revealed that auranofin alone and in combination with standard drugs significantly decreased the bioburden in zebrafish infection model as compared to control. The molecular docking study have shown good interaction of auranofin with penicillin binding protein (2Y2M), topoisomerase (3TTZ), UDP-3-O-[3- hydroxymyristoyl] N-acetylglucosaminedeacetylase (3UHM), cell adhesion protein (4QRK), β-lactamase (5CTN) and arylsulphatase (1HDH) enzyme as that of reference ligand which indicate multimodal mechanism of action of auranofin. Finally, MTT assay has shown non-cytotoxic effect of auranofin. Conclusion: In conclusion, auranofin in combination with existing antibiotics could be developed as a broad spectrum antibacterial agent; however, further studies are required to confirm its safety and efficacy. This study provides possibility of use of auranofin apart from its established therapeutic indication in combination with existing antibiotics to tackle the problem of resistance.


2010 ◽  
Vol 1 (1) ◽  
pp. 35-38 ◽  
Author(s):  
Ryan Dosselli ◽  
Marina Gobbo ◽  
Erika Bolognini ◽  
Sandro Campestrini ◽  
Elena Reddi

2002 ◽  
Vol 46 (5) ◽  
pp. 1262-1268 ◽  
Author(s):  
Qing Li ◽  
Jean Y. Lee ◽  
Rosario Castillo ◽  
Mark S. Hixon ◽  
Catherine Pujol ◽  
...  

ABSTRACT Enzyme-catalyzed therapeutic activation (ECTA) is a novel prodrug strategy to overcome drug resistance resulting from enzyme overexpression. β-Lactamase overexpression is a common mechanism of bacterial resistance to β-lactam antibiotics. We present here the results for one of the β-lactamase ECTA compounds, NB2001, which consists of the antibacterial agent triclosan in a prodrug form with a cephalosporin scaffold. Unlike conventional β-lactam antibiotics, where hydrolysis of the β-lactam ring inactivates the antibiotic, hydrolysis of NB2001 by β-lactamase releases triclosan. Evidence supporting the proposed mechanism is as follows. (i) NB2001 is a substrate for TEM-1 β-lactamase, forming triclosan with a second-order rate constant (k cat/Km ) of greater than 77,000 M−1 s−1. (ii) Triclosan is detected in NB2001-treated, β-lactamase-producing Escherichia coli but not in E. coli that does not express β-lactamase. (iii) NB2001 activity against β-lactamase-producing E. coli is decreased in the presence of the β-lactamase inhibitor clavulanic acid. NB2001 was similar to or more potent than reference antibiotics against clinical isolates of Staphylococcus aureus (including MRSA), Staphylococcus epidermidis, Streptococcus pneumoniae, vancomycin-resistant Enterococcus faecalis, Moraxella catarrhalis and Haemophilus influenzae. NB2001 is also active against Klebsiella pneumoniae, Enterobacter aerogenes, and Enterobacter cloacae. The results indicate that NB2001 is a potent, broad-spectrum antibacterial agent and demonstrate the potential of ECTA in overcoming β-lactamase-mediated resistance.


Author(s):  
Caio Rodrigues da Silva ◽  
Milena Guedes Maniero ◽  
Susanne Rath ◽  
José Roberto Guimarães

AbstractFlumequine is a broad-spectrum antibacterial agent of the quinolone class widely used as veterinary drug in food-producing animals. It is considered as pseudo-persistent compound continuously introduced into the environment and its presence in the environment may contribute to the development of drug resistant bacterial strains. In this study antibacterial activity removal during flumequine degradation by UV/H


2020 ◽  
Vol 8 (15) ◽  
pp. 3010-3015
Author(s):  
Yanbin Sun ◽  
Xianwen Wang ◽  
Linxin Fan ◽  
Xianli Xie ◽  
Zhaohua Miao ◽  
...  

Monodisperse chromogenic amylose–iodine nanoparticles were developed as an efficient broad-spectrum antibacterial agent under the assistance of near-infrared laser irradiation.


PLoS ONE ◽  
2017 ◽  
Vol 12 (9) ◽  
pp. e0183457 ◽  
Author(s):  
Abiodun D. Ogunniyi ◽  
Manouchehr Khazandi ◽  
Andrew J. Stevens ◽  
Sarah K. Sims ◽  
Stephen W. Page ◽  
...  

2015 ◽  
Vol 96 ◽  
pp. 152-161 ◽  
Author(s):  
M.S. Nieto-Bobadilla ◽  
F. Siepmann ◽  
M. Djouina ◽  
L. Dubuquoy ◽  
N. Tesse ◽  
...  

2012 ◽  
Vol 15 (1) ◽  
pp. 132-142 ◽  
Author(s):  
Xiaoyan Xue ◽  
Xiaoqing Chen ◽  
Xinggang Mao ◽  
Zheng Hou ◽  
Ying Zhou ◽  
...  

1963 ◽  
Vol 1 (8) ◽  
pp. 29-30

Methenamine mandelate (Mandelamine - Warner), a combination of methenamine and mandelic acid, is promoted as a broad-spectrum antibacterial agent that can be used against chronic or recurrent urinary infections without the appearance of resistant strains. In the urine, the drug yields formaldehyde and mandelic acid, both of which act only in the urine and not at all in the tissues of the urinary tract. Mandelic acid has less antibacterial effect than formaldehyde, but causes some acidification of the urine. Each component requires a pH of 5. 5 or less in the urine for even moderate antibacterial activity, and a supplementary acidifying agent is usually necessary.


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