Abstract：
:A series of 32 piperazine-linked bisbenzamidines (and related analogues) were analysed for their in vitro and in vivo trypanocidal activity against a drug-sensitive strain of Trypanosoma brucei brucei and a drug-resistant strain of Trypanosoma brucei rhodesiense. The compounds showed similar potencies against both strains. The most potent compounds were bisbenzamidines substituted at the amidinium nitrogens with a linear pentyl group (8, inhibitory concentration for 50% (IC(50))=1.7-3.0 nM) or cyclic octyl group (17, IC(50)=2.3-4.6 nM). Replacement of the diamidine groups with diamidoxime groups resulted in a prodrug (22) that was effective orally against T. b. brucei-infected mice. Three compounds (7, 11 and 15) provided 100% cure when administered parenterally. The results indicate that the nature of the substituents at the amidinium nitrogens of bisbenzamidines strongly influence their trypanocidal activity.
journal_name
Int J Antimicrob Agentsjournal_title
International journal of antimicrobial agentsauthors
Huang TL,Bacchi CJ,Kode NR,Zhang Q,Wang G,Yartlet N,Rattendi D,Londono I,Mazumder L,Vanden Eynde JJ,Mayence A,Donkor IOdoi
10.1016/j.ijantimicag.2007.07.021subject
Has Abstractpub_date
2007-12-01 00:00:00pages
555-61issue
6eissn
0924-8579issn
1872-7913pii
S0924-8579(07)00351-2journal_volume
30pub_type
杂志文章abstract：:The use of biomarkers might help to avoid antibiotic misuse and overuse and to curb the rising incidence of microbial resistance. Amongst >100 biomarkers proposed for use as infection/sepsis markers, procalcitonin is the most frequently evaluated. It has been tested in 11 randomised controlled trials with more than 35...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章,评审
doi：10.1016/j.ijantimicag.2010.11.009
更新日期：2010-12-01 00:00:00
abstract：OBJECTIVES:This study aimed to explore the genetic diversity of Streptococcus pneumoniae isolates in a Tunisian pneumology hospital. METHODS:A total of 141 S. pneumoniae strains isolated between 2009-2016 in the microbiology laboratory at A. Mami Hospital of Pneumology were investigated. Antimicrobial susceptibility t...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
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abstract：:D-Alanylgriseoluteic acid (AGA) is a potent antimicrobial phenazine compound produced by Pantoea agglomerans (Erwinia herbicola) Eh1087. Susceptibility tests against a range of microbes indicated that AGA had a broad spectrum of antimicrobial activity and was particularly active against Gram-positive pathogens. Compar...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2006.08.028
更新日期：2007-01-01 00:00:00
abstract：:Renal, liver, heart and lung transplantation are now considered to be the standard therapeutic interventions in patients with end-stage organ failure. Infectious complications following solid organ transplantation (SOT) are relatively common owing to the transplant recipient's overall immunosuppressed status. The inci...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章,评审
doi：10.1016/S0924-8579(08)70017-7
更新日期：2008-11-01 00:00:00
abstract：:The purpose of this study was to characterise the metallo-beta-lactamase VIM-6 and the genetic environment of the bla(VIM-6) gene. The bla(VIM-6) gene was cloned into an Escherichia coli expression system and the purified VIM-6 enzyme was obtained. VIM-6 has an isoelectric point of 4.9 and a molecular weight of 28.368...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2008.05.017
更新日期：2008-11-01 00:00:00
abstract：:Demonstration of efflux of ethidium bromide (EtBr) has been made for over 30 bacterial species, usually by showing enhanced efflux in multidrug-resistant strains that was then abolished by inactivating efflux pumps. Here we present a relatively simple automated method that employs EtBr as an efflux pump substrate for ...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2007.12.015
更新日期：2008-05-01 00:00:00
abstract：:The novel ketolide telithromycin (formerly HMR-3647) was tested against a collection of pneumococci of varying sensitivity to erythromycin and clindamycin, isolated in geographically diverse UK hospitals. Telithromycin was highly active against erythromycin-susceptible pneumococci, the MIC(90) being 0.015 mg/l. Erythr...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/s0924-8579(01)00346-6
更新日期：2001-07-01 00:00:00
abstract：:The resistance patterns of Escherichia coli in untreated (raw) urban wastewater (UW) was monitored by repeated sampling during 1 year. Comparison with data from wastewater samples collected from hospital wastewater (HW) in the same urban area was made. A total of 1326 E. coli isolates from 17 UW samples and 451 isolat...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2014.09.016
更新日期：2015-01-01 00:00:00
abstract：:The effect of subinhibitory concentrations of amikacin and ciprofloxacin on the hydrophobicity and adherence to uroepithelial cells of Escherichia coli strains was investigated. The hydrophobicity of the tested strains was evaluated by the bacterial adherence to hydrocarbon-xylene test and by the salt aggregation test...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2007.01.007
更新日期：2007-06-01 00:00:00
abstract：:Skin and soft tissue infections (SSTIs) are common and range in severity from minor, self-limiting, superficial infections to life-threatening diseases requiring all the resources of modern medicine. The classification of SSTIs can be based on the anatomical site, clinical severity or microbial cause, but some classif...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章,评审
doi：10.1016/S0924-8579(09)70541-2
更新日期：2009-07-01 00:00:00
abstract：:Of the 16,024 patients hospitalized from January 1995 to October 1997, 397 (2.4%) acquired nosocomial pneumonia and the aetiological agent was defined in 101 (25%). About 82% developed late onset pneumonia (>7 days of hospitalization). The site of isolation of microorganisms was bronchoalveolar lavage (BAL) (49%), blo...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/s0924-8579(00)00316-2
更新日期：2001-02-01 00:00:00
abstract：:Gatifloxacin, grepafloxacin, moxifloxacin and trovafloxacin are fluoroquinolones with enhanced Gram-positive activity while retaining broad-spectrum activity against Gram-negative pathogens. Levofloxacin and ciprofloxacin are older quinolones with broad activity against Gram-negative pathogens and borderline activity ...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/s0924-8579(99)00143-0
更新日期：2000-02-01 00:00:00
abstract：:In this study, the prevalence and characteristics of metallo-β-lactamase (MBL)-producing Pseudomonas aeruginosa isolates in South Korea were investigated. Among 215 P. aeruginosa isolates collected from eight hospitals, 77 (35.8%) and 72 (33.5%) were resistant to imipenem and meropenem, respectively. Of the 77 imipene...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2017.01.023
更新日期：2017-06-01 00:00:00
abstract：:Helicobacter infection, one of the most common bacterial infections in man worldwide, is a type 1 carcinogen and the most important risk factor for gastric cancer. Helicobacter pylori bacterial factors, components of the host genetics and immune response, dietary cofactors and decreased acid secretion resulting in bac...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2008.10.032
更新日期：2009-05-01 00:00:00
abstract：:Acinetobacter baumannii has emerged as an important nosocomial pathogen owing to its increasing resistance to most, if not all, antibiotics in clinical use. We recently reported the occurrence of extensively drug-resistant (XDR) A. baumannii isolates in a Malaysian tertiary hospital. The genome of one of these XDR iso...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2014.10.015
更新日期：2015-02-01 00:00:00
abstract：:The clinical significance and management of asymptomatic bacteriuria (ASB) differs according to different groups of patients. ASB requires antibiotic treatment in pregnant women, children aged 5-6 years and prior to invasive genitourinary procedures. However, there is a consensus that ASB in the elderly, healthy schoo...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章,评审
doi：10.1016/s0924-8579(03)00248-6
更新日期：2003-10-01 00:00:00
abstract：:Meticillin-resistant Staphylococcus aureus (MRSA), both hospital-acquired and community-acquired MRSA (CA-MRSA) strains, have increased in frequency in the last few years, reaching epidemic dimensions. This review discusses several clinical forms of staphylococcal infection leading to bacteraemia in a high proportion ...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章,评审
doi：10.1016/j.ijantimicag.2008.06.006
更新日期：2008-11-01 00:00:00
abstract：:Klebsiella pneumoniae carbapenemase-producing K. pneumoniae (KPC-KP) bloodstream infections (BSIs) are related to high mortality rates, and combination therapy has been associated with lower mortality in patients treated mostly with colistin. There is a paucity of studies addressing polymyxin B (PMB) treatment for KPC...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2018.10.010
更新日期：2019-02-01 00:00:00
abstract：:The purpose of this study was (i) to determine the optimal dosage of teicoplanin for each patient group stratified by renal function and weight based on a population pharmacokinetic model and observed distribution of patient characteristics and (ii) to develop new simplified dosing regimens designed to achieve 15-30 μ...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2012.05.025
更新日期：2012-10-01 00:00:00
abstract：:Modifications of the immune response have been reported for a number of antimicrobial agents following both in vivo and in vitro experiments. Present results were obtained from in vitro incubated human polymorphonuclear cells (PMN) and monocytes treated with meropenem, a novel carbapenem antibiotic. Only the highest c...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/0924-8579(94)00042-s
更新日期：1995-04-01 00:00:00
abstract：:The aim of this study was to investigate recurrent infections in individual patients caused by extended-spectrum β-lactamase and plasmid AmpC β-lactamase-producing Escherichia coli (ESBL/pAmpC-Ec) isolates with >12-month interval. The Danish national collection of ESBL/pAmpC-Ec isolates collected from January 2014 thr...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2020.106041
更新日期：2020-07-01 00:00:00
abstract：:Antimicrobial peptides (AMPs) are produced by all forms of living organisms and represent a novel class of antibiotics to treat infectious diseases. In this study, 29 AMPs of varying length and characteristics were synthesised chemically and were evaluated for their ability to inhibit the growth of Bacillus globigii, ...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2010.06.038
更新日期：2010-10-01 00:00:00
abstract：:The beta-lactamases of five strains each of Y. aldovae and "Y. ruckeri", and 10 strains each of Y. bercovieri and Y. frederiksenii were examined phenotypically and genetically. Beta-lactamase activity and induction assays and SDS-PAGE were applied for phenotypic characterization of these enzymes. Genotypically, PCR ex...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2004.08.020
更新日期：2005-06-01 00:00:00
abstract：:The feasibility of using colicins to create an antimicrobial lubricant to prevent extraluminal catheter contamination during urinary catheter insertion was assessed. Levels of resistance of uropathogenic Escherichia coli to antibiotics and colicins were compared. The results showed that antibiotics and colicins posses...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2019.07.004
更新日期：2019-11-01 00:00:00
abstract：:Many studies have elucidated the risk factors associated with peri-operative infection following head and neck cancer surgery (HNS), the implications of infection for total treatment cost, and the clinical benefits of successful antimicrobial prophylaxis. The most appropriate antibiotic use is achieved by focusing on ...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章,评审
doi：10.1016/s0924-8579(99)00088-6
更新日期：1999-08-01 00:00:00
abstract：:An open, multicentre study was performed in hospital in-patients at a total of 12 German hospitals to investigate the efficacy and tolerability of sulbactam combined with mezlocillin, piperacillin or cefotaxime in severe bacterial infections. A total of 155 patients were recruited into the study, of whom 48 were suffe...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：
更新日期：1996-04-01 00:00:00
abstract：:Many studies have demonstrated that sub-minimum inhibitory concentrations (sub-MICs) of antimicrobial agents can inhibit bacterial biofilm formation. However, the mechanisms by which antimicrobial agents at sub-MICs inhibit biofilm formation remain unclear. At present, most studies are focused on Gram-negative bacteri...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2012.01.009
更新日期：2012-05-01 00:00:00
abstract：:Cellulitis is a commonly seen clinical syndrome that is most often associated with beta-haemolytic streptococci and Staphylococcus aureus. Several medical conditions and a variety of procedures can predispose to the development of cellulitis by a common mechanism: venous and lymphatic compromise. The precise pathophys...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/s0924-8579(99)00169-7
更新日期：2000-03-01 00:00:00
abstract：:Between November 2001 and November 2004, 231 Escherichia coli isolates resistant to beta-lactam antibiotics were identified. In 14 isolates, bla(TEM-24) (2 isolates), bla(TEM-52) (5 isolates) and bla(TEM-26) (7 isolates) were identified. In 145 E. coli isolates with the same M13 fingerprinting profile and the same res...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/j.ijantimicag.2006.08.002
更新日期：2006-10-01 00:00:00
abstract：:The in vitro activity of ciprofloxacin, ofloxacin, levofloxacin and moxifloxacin against strains of Mycobacterium tuberculosis was studied. Moxifloxacin and levofloxacin showed the greatest activity having an MIC(90) of 1 mg/l. The MIC(90) for ofloxacin was 2 mg/l and for ciprofloxacin 4 mg/l. Further studies should b...
journal_title：International journal of antimicrobial agents
pub_type： 杂志文章
doi：10.1016/s0924-8579(00)00337-x
更新日期：2001-03-01 00:00:00
