Global Surveillance Through PROTEKT: The First Year.
Authors: Grüneberg RN
Abstract
The increasing antimicrobial resistance amongst bacterial pathogens causing community-acquired respiratory tract infections (CARTIs) necessitates surveillance at the local, regional, national and international levels to provide information to guide empiric antimicrobial therapy. PROTEKT (Prospective Resistant Organism Tracking and Epidemiology for the Ketolide Telithromycin) is a longitudinal, global, multicenter surveillance study designed to monitor the worldwide development of antimicrobial resistance and disseminate up-to-date information via the internet to assist in th...
Source: Journal of Chemotherapy - November 2, 2016 Category: Cancer & Oncology Tags: J Chemother Source Type: research
The Rise of Fluoroquinolone Resistance: Fact or Fiction.
Authors: Ferraro MJ
Abstract
Fluoroquinolone antibiotics have been available since the 1980s when ciprofloxacin and norfloxacin were licensed. Structural revisions of the quinolone molecule have provided new compounds that were well suited to the treatment of upper and lower community-acquired respiratory tract infections, having good activity against Streptococcus pneumoniae. Nevertheless, it was only a matter of time before the pneumococcus developed effective resistance against these new agents. There are populations of fluoroquinolone-resistant S. pneumoniae and, more worryingly, many of these strains ...
Source: Journal of Chemotherapy - November 2, 2016 Category: Cancer & Oncology Tags: J Chemother Source Type: research
Risk of sensorineural hearing loss with macrolide antibiotics: A nested case ‐control study
ConclusionA significant association between SNHL and macrolide use was likely due to confounding by indication for antibiotic treatment because the risk was also observed with fluoroquinolones and amoxicillin, antibiotics with no known ototoxic potential. Therefore, there does not appear to be an increased risk of SNHL in patients treated with macrolide antibiotics.
Level of Evidence3b. Laryngoscope, 2016 (Source: The Laryngoscope)
Source: The Laryngoscope - August 5, 2016 Category: ENT & OMF Authors: Mahyar Etminan, Brian D. Westerberg, Frederick K. Kozak, Michael Y. Guo, Bruce C. Carleton Tags: Otology/Neurotology Source Type: research
Results from the Solithromycin International Surveillance Program (2014).
In conclusion, solithromycin demonstrated potent activity against global and contemporary (2014) pathogens that represent the major causes of community-acquired bacterial pneumonia. These data support the continued clinical development of solithromycin for the treatment of this important indication.
PMID: 27044551 [PubMed - as supplied by publisher] (Source: Antimicrobial Agents and Chemotherapy)
Source: Antimicrobial Agents and Chemotherapy - April 3, 2016 Category: Microbiology Authors: Farrell DJ, Flamm RK, Sader HS, Jones RN Tags: Antimicrob Agents Chemother Source Type: research
The role of solithromycin in the management of bacterial community-acquired pneumonia.
Authors: Van Bambeke F, Tulkens PM
Abstract
The fluoroketolide solithromycin is 2-fold more potent in vitro than telithromycin against pneumococci (including macrolide-resistant strains) and Haemophilus influenzae and very active on pathogens causing atypical pneumonia. In contrast, it is a 30-fold less potent inhibitor of nicotinic receptors incriminated in telithromycin toxicity. In Phase II/III trials, oral solithromycin once-daily (800 mg on day 1; 400 mg on days 2-5) proved effective and safe when compared to respiratory fluoroquinolones for the treatment of community-acquired bacterial pneumonia (CAB...
Source: Expert Review of Anti-Infective Therapy - February 14, 2016 Category: Infectious Diseases Tags: Expert Rev Anti Infect Ther Source Type: research
Synthesis and antibacterial evaluation of novel 4″-glycyl linked quinolyl-azithromycins with potent activity against macrolide-resistant pathogens.
Abstract
A new azithromycin-based series of antibacterial macrolones is reported, which features the use of a 4″-ester linked glycin for tethering the quinolone side chain to the macrolide scaffold. Among the analogs prepared, compounds 9e and 22f with a quinolon-6-yl moiety were found to have potent and well-balanced activity against clinically important respiratory tract pathogens, including erythromycin-susceptible and MLSB resistant strains of Streptococcus pneumoniae, Streptococcus pyogenes, and Haemophilus influenzae. In addition, potential lead compounds 9e and 22f demonstrated outstanding levels ...
Source: Bioorganic and Medicinal Chemistry - February 1, 2016 Category: Chemistry Authors: Pavlović D, Mutak S Tags: Bioorg Med Chem Source Type: research
Ketolide agents HMR 3004 and HMR 3647 (telithromycin) inhibit the growth of Plasmodium falciparum in vitro
Conclusion: The results indicate lack of cross-resistance between the ketolide compounds and chloroquine, implying presence of a drug target different from that of chloroquine. The particular drug target has still to be investigated but the stage-specific results indicate that it is expressed in all parasite growth phases. These observations demonstrate the anti-malarial potential of the ketolide antimicrobial agents.Key words: Chloroquine, ketolides, macrolides, malaria, Plasmodium falciparum. (Source: African Health Sciences)
Source: African Health Sciences - January 23, 2016 Category: African Health Source Type: research
Investigation of avalanche photodiodes radiation hardness for baryonic matter studies
Abstract
Modern avalanche photodiodes (APDs) with high gain are good device candidates for light readout from detectors applied in relativistic heavy ion collisions experiments. The results of the investigations of the APDs properties from Zecotek, Ketek and Hamamatsu manufacturers after irradiation using secondary neutrons from cyclotron facility U120M at NPI of ASCR in Řež are presented. The results of the investigations can be used for the design of the detectors for the experiments at NICA and FAIR. (Source: Physics of Particles and Nuclei Letters)
Source: Physics of Particles and Nuclei Letters - January 1, 2016 Category: Physics Source Type: research
[Macrolide-lincosamide-streptogramin B (MLSB) resistance phenotypes in clinical Staphylococcus isolates and investigation of telithromycin activity].
In conclusion, clindamycin is still an effective antibiotic for the treatment of staphylococcal infections in our hospital, however, 34% resistance rate against telithromycin may limit the use of this agent which is an alternative for the treatment of infections caused by clindamycin and erythromycin-resistant strains.
PMID: 25052113 [PubMed - indexed for MEDLINE] (Source: Mikrobiyoloji Bulteni)
Source: Mikrobiyoloji Bulteni - December 2, 2015 Category: Microbiology Tags: Mikrobiyol Bul Source Type: research
Type 3 secretion-dependent sensitivity of Escherichia coli O157 to specific ketolides.
In this study we screened established bioactive compounds for any that could repress T3SS expression in enterohemorrhagic Escherichia coli (EHEC) O157. The ketolides, telithromycin and subsequently solithromycin both demonstrated repressive effects on expression of the bacterial T3SS at sub-minimum inhibitory (sub-MIC) concentrations, leading to significant reductions in bacterial binding and actin-rich pedestal formation on epithelial cells. Pre-incubation of epithelial cells with solithromycin resulted in significantly less attachment of E. coli O157. Moreover, bacteria expressing the T3SS were more susceptible to solith...
Source: Antimicrobial Agents and Chemotherapy - November 2, 2015 Category: Microbiology Authors: Fernandez-Brando R, Yamaguchi N, Tahoun A, McAteer SP, Gillespie T, Wang D, Argyle SA, Palermo MS, Gally DL Tags: Antimicrob Agents Chemother Source Type: research
Species specificity of a ribosome from a pathogen [Biophysics and Computational Biology]
The emergence of bacterial multidrug resistance to antibiotics threatens to cause regression to the preantibiotic era. Here we present the crystal structure of the large ribosomal subunit from Staphylococcus aureus, a versatile Gram-positive aggressive pathogen, and its complexes with the known antibiotics linezolid and telithromycin, as well as with a... (Source: Proceedings of the National Academy of Sciences)
Source: Proceedings of the National Academy of Sciences - October 27, 2015 Category: Science Authors: Eyal, Z., Matzov, D., Krupkin, M., Wekselman, I., Paukner, S., Zimmerman, E., Rozenberg, H., Bashan, A., Yonath, A. Tags: PNAS Plus Source Type: research
RlmCD-mediated U747 methylation promotes efficient G748 methylation by methyltransferase RlmAII in 23S rRNA in Streptococcus pneumoniae; interplay between two rRNA methylations responsible for telithromycin susceptibility
Adenine at position 752 in a loop of helix 35 from positions 745 to 752 in domain II of 23S rRNA is involved in binding to the ribosome of telithromycin (TEL), a member of ketolides. Methylation of guanine at position 748 by the intrinsic methyltransferase RlmAII enhances binding of telithromycin (TEL) to A752 in Streptococcus pneumoniae. We have found that another intrinsic methylation of the adjacent uridine at position 747 enhances G748 methylation by RlmAII, rendering TEL susceptibility. U747 and another nucleotide, U1939, were methylated by the dual-specific methyltransferase RlmCD encoded by SP_1029 in S. pneumoniae....
Source: Nucleic Acids Research - October 14, 2015 Category: Research Authors: Shoji, T., Takaya, A., Sato, Y., Kimura, S., Suzuki, T., Yamamoto, T. Tags: RNA Source Type: research
Total Synthesis of Desmethyl Macrolide Antibiotics
SynlettDOI: 10.1055/s-0034-1381047Macrolide antibiotics occupy a special place in the history of organic chemistry and medicine. This account chronicles the evolution of our approach that ultimately led to the successful total syntheses of four desmethyl (i.e., Me → H) analogues of telithromycin, a semisynthetic derivative of the flagship macrolide antibiotic, erythromycin.1 Introduction2 Project Rationale and Retrosynthetic Analysis3 Lessons Learned from the Total Synthesis of 4,8,10-Tridesmethyl Telithromycin4 Total Synthesis of 4,10-Didesmethyl Telithromycin5 Total Synthesis of 4,8-Didesmethyl Telithromycin6 Tot...
Source: Synlett - September 3, 2015 Category: Chemistry Authors: Andrade, Rodrigo B. Tags: account Source Type: research
Inducible expression of (B) by the ketolides telithromycin and cethromycin
Sir, Ketolides have generally been considered to be non-inducers of the resistance conferred by erm genes. A previous study reported that erm(B) was not induced by the ketolide telithromycin [1]. Inconsistent with this earlier result, however, it was subsequently reported that dimethylation at A2058 of 23S rRNA in a strain of Streptococcus pneumoniae with erm(B) was increased in the presence of telithromycin [2]. A recent study also showed that the ketolides telithromycin and cethromycin caused ribosome stalling at the regulatory region of erm(B) in an Escherichia coli cell-free system [3]. (Source: International Journal o...
Source: International Journal of Antimicrobial Agents - June 3, 2015 Category: Drugs & Pharmacology Authors: Byoungduck Park, Yu-Hong Min Tags: Letter to the Editor Source Type: research
Novel gentamicin resistance genes in Campylobacter isolated from humans and retail meats in the USA
Conclusions
This study demonstrated that several new aminoglycoside resistance genes underlie the recent emergence of gentamicin-resistant Campylobacter, and that, in addition to contaminated retail chicken, other sources have also contributed to gentamicin-resistant Campylobacter infections in humans. (Source: Journal of Antimicrobial Chemotherapy)
Source: Journal of Antimicrobial Chemotherapy - April 13, 2015 Category: Microbiology Authors: Zhao, S., Mukherjee, S., Chen, Y., Li, C., Young, S., Warren, M., Abbott, J., Friedman, S., Kabera, C., Karlsson, M., McDermott, P. F. Tags: Original research Source Type: research
