Abstract：
:The aim of this study was to screen lead compounds exhibiting potent in vitro antimicrobial activity against multidrug-resistant (MDR) Acinetobacter baumannii strains from a library of chemical compounds. In a high-throughput screening analysis of 7520 compounds representative of 340,000 small molecules, two 4H-4-oxoquinolizine compounds were the most active against A. baumannii ATCC 17978. Subsequent selection and analysis of 70 4H-4-oxoquinolizine compounds revealed that the top 7 compounds were extremely active against extensively drug-resistant (XDR) A. baumannii isolates. These compounds commonly carried a 1-cyclopropyl-7-fluoro-4-oxo-4H-quinolizine-3-carboxylic acid core structure but had different C-8 and/or C-9 moieties. Minimum inhibitory concentrations (MICs) of the seven compounds against fluoroquinolone-resistant A. baumannii isolates were found to be in the range of 0.02-1.70 µg/mL regardless of the mutation types in the quinolone resistance-determining region (QRDR) of GyrA and ParC. Cytotoxicity of the seven compounds was observed in HeLa and U937 cells at a concentration of 50 µg/mL, which was >32.5- to 119-fold higher than the MIC90 for A. baumannii isolates. In conclusion, novel 4H-4-oxoquinolizine compounds represent a promising scaffold on which to develop antimicrobial agents against drug-resistant A. baumannii strains.
journal_name
Int J Antimicrob Agentsjournal_title
International journal of antimicrobial agentsauthors
Na SH,Jeon H,Kim YJ,Kwon HI,Selasi GN,Nicholas A,Yun CS,Lee SH,Lee JCdoi
10.1016/j.ijantimicag.2016.10.008subject
Has Abstractpub_date
2017-01-01 00:00:00pages
107-111issue
1eissn
0924-8579issn
1872-7913pii
S0924-8579(16)30344-2journal_volume
49pub_type
杂志文章abstract：:In Europe, a novel mecA homologue - mecC (formerly mecALGA251) - has emerged recently in staphylococci from animals, humans and the environment. This paper reports the first occurrence of the mecC gene in Staphylococcus sciuri from cows and manure in Tunisia and Africa. Forty-nine coagulase-negative staphylococci (CNS...
journal_title：International journal of antimicrobial agents
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abstract：:Piperacillin plasma concentrations are known to vary between critically ill patients. However, there are no comprehensive data on the variability of antibiotic concentrations within the same patient. The purpose of this study was to investigate the adequacy of dosing during an entire 7-day antibiotic course and to inv...
journal_title：International journal of antimicrobial agents
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abstract：OBJECTIVES:This study reported a hospital outbreak due to an extensively drug-resistant (XDR) OXA-72-producing strain of Acinetobacter baumannii (A. baumannii). METHODS AND RESULTS:The isolates were found to be genotypically indistinguishable by whole-genome multiple locus sequence typing, and to belong to the interna...
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章,评审
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abstract：:Candida spp., especially Candida albicans, is one of the main colonisers of the oral cavity. Due to its ability to form biofilms, it can be implicated in dental caries, periodontal disease and denture stomatitis. Microbial cells in biofilms are minimally impacted by conventional drugs. The aim of this study was to fin...
journal_title：International journal of antimicrobial agents
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journal_title：International journal of antimicrobial agents
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journal_title：International journal of antimicrobial agents
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更新日期：2006-06-01 00:00:00
abstract：:The antimicrobial activity against Clostridium difficile of 109 lactic acid bacteria (LAB) isolated from 32 healthy Korean infants was measured. The ability to show similar activity against Escherichia coli O157:H7 and Staphylococcus aureus was also looked for. Twelve of the 109 LAB showed activity against C. difficil...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
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journal_title：International journal of antimicrobial agents
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
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abstract：:Carbapenem-resistant Enterobacterales have become a major public-health issue worldwide. Here we report an outbreak caused by a clonal multidrug-resistant Proteus mirabilis strain producing VIM-4 metallo-β-lactamase (MBL) and TEM-2 β-lactamase in a Greek tertiary-care hospital. From July 2015 to February 2016, 27 imip...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
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更新日期：2020-08-01 00:00:00
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章,评审
doi：10.1016/S0924-8579(08)70023-2
更新日期：2008-11-01 00:00:00
abstract：:Globally, antibiotic resistance continues to be an increasing problem. The emergence of methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococci (VRE), and extended spectrum beta-lactamase-producing Enterobacteriaceae has seriously reduced the number of empirical agents suitable for selecte...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章,评审
doi：10.1016/S0924-8579(09)70003-2
更新日期：2008-12-01 00:00:00
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2019.11.013
更新日期：2020-01-01 00:00:00
abstract：:Wide-spectrum quinolones such as moxifloxacin and levofloxacin as well as high-order cephalosporins such as cefoperazone and cefepime have increased antimicrobial activity. However, little is known about their distribution in fetal blood. Therefore, the aim of this study was to measure and compare maternal and fetal b...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2010.03.011
更新日期：2010-08-01 00:00:00
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2019.08.017
更新日期：2019-11-01 00:00:00
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2006.03.023
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/s0924-8579(97)00041-1
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章,评审
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
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更新日期：2001-05-01 00:00:00
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
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更新日期：2014-05-01 00:00:00
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2005.02.019
更新日期：2005-07-01 00:00:00
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2015.10.016
更新日期：2016-01-01 00:00:00
abstract：:Carbapenem-resistant Enterobacteriaceae (CRE) are among the most difficult to treat emerging multidrug-resistant organisms. Major limitations exist in surveillance needed to address CRE, particularly in areas with inadequate resources. We utilised optimised strategies to search for data on carbapenem susceptibility of...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章,评审
doi：10.1016/j.ijantimicag.2018.05.019
更新日期：2018-09-01 00:00:00
abstract：:The ability of antibiotics used in bronchopulmonary infections in cystic fibrosis (CF) patients to prevent Pseudomonas aeruginosa early biofilm formation was studied using a biofilm microtitre assay with 57 non-mucoid P. aeruginosa isolates (44 first colonisers and 13 recovered during the initial intermittent colonisa...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2012.04.006
更新日期：2012-08-01 00:00:00
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journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/s0924-8579(00)00277-6
更新日期：2000-12-01 00:00:00
abstract：:Community-acquired pneumonia (CAP) is still one of the leading causes of mortality and morbidity. The most common bacterial cause of CAP is Streptococcus pneumoniae. The increase in antimicrobial resistance has raised concerns about the efficacy of available therapies, and a call for the reassessment of both existing ...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章,评审
doi：10.1016/j.ijantimicag.2004.08.006
更新日期：2004-11-01 00:00:00
abstract：:In November 2015, the first plasmid-encoded colistin resistance gene, mcr-1, was described in animals and in humans in China. Subsequently, a multitude of further studies was performed and quite recently the global spread of mcr-1 as well as the occurrence of a new gene variant, mcr-2, was reported. To obtain an overv...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2017.03.007
更新日期：2017-08-01 00:00:00
abstract：:The impact of extended-spectrum β-lactamase (ESBL)-producing Enterobacteriaceae of food animal origins on human health has caught considerable attention worldwide. Intestinal Escherichia coli obtained from healthy food animals (pigs, cattle and poultry) in China were tested for the presence of ESBL genes. CTX-M-produc...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2011.12.001
更新日期：2012-04-01 00:00:00
