Abstract:
:The search for new nucleoside analogue compounds targeting the virally encoded reverse transcriptase was developed by modifying the nucleoside structure to create inhibitor compounds. In this review, the structure-activity relationship of antiviral compounds synthesised from the naturally existing cytosine deoxyribonucleoside (dC) was evaluated. The line of research starting from dC led to the synthesis of 2',3'-dideoxycytidine (ddC; zalcitabine), 2',3'-dideoxy-3'-thiacytidine (3TC; lamivudine) and 2',3'-dideoxy-5-fluoro-3'-thiacytidine (FTC; emtricitabine) and looks very interesting because each product comes from a single small change in the chemical structure of the former compound, resulting in a progressive improvement in terms of activity, pharmacokinetics, tolerability and emergence of resistance.
journal_name
Int J Antimicrob Agentsjournal_title
International journal of antimicrobial agentsauthors
Scaglione F,Berrino Ldoi
10.1016/j.ijantimicag.2011.11.013subject
Has Abstractpub_date
2012-06-01 00:00:00pages
458-63issue
6eissn
0924-8579issn
1872-7913pii
S0924-8579(12)00002-7journal_volume
39pub_type
杂志文章abstract::Complicated and recurrent urinary tract infections present intriguing clinical management problems. The underlying conditions in patients with complicated urinary tract infections are anatomical abnormalities of the genitourinary tract, neurologic disorders resulting in urinary stasis, obstruction, instrumentation, su...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/0924-8579(94)90019-1
更新日期:1994-07-01 00:00:00
abstract::A total of 89 patients, (>18 years), with symptoms of chronic prostatitis and inflammatory findings as well as the presence of Chlamydia trachomatis confirmed by DNA/RNA DIGENE hybridization method and/or by isolation, McCoy culture and Lugol stain in expressed prostatic secretion or in voided bladder urine collected ...
journal_title:International journal of antimicrobial agents
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1016/s0924-8579(03)00056-6
更新日期:2003-05-01 00:00:00
abstract::This study aimed to identify factors associated with virological response (VR) to raltegravir (RAL)-containing regimens in 468 treatment-experienced but integrase inhibitor-naive HIV-1 patients receiving a RAL-containing regimen. VR was defined at Month 6 (M6) as HIV-1 RNA viral load (VL) <50 copies/mL. The impacts on...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2013.02.016
更新日期:2013-07-01 00:00:00
abstract::In vitro and clinical data were analysed to evaluate the susceptibility profile of itraconazole in light of the new cut-off points. The in vitro activity of itraconazole was compared with that of eight comparators against 119 Candida bloodstream isolates from 2015 to 2018. Minimum inhibitory concentrations (MICs) were...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2019.06.019
更新日期:2019-10-01 00:00:00
abstract::Fresh clinical isolates collected from November 1, 1992 through November 1, 1993, were tested by agar dilution against 26 different antimicrobial agents including FK037 and l-ofloxacin. Among the 10 040 organisms tested were Staphylococcus aureus (n = 1222), methicillin-resistant Staphylococcus aureus (MRSA, n = 455),...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/0924-8579(95)00039-9
更新日期:1996-04-01 00:00:00
abstract::Advanced molecular typing methods have greatly expanded the taxonomy of Mycobacterium avium complex (MAC) species; however, little is known about the epidemiology and clinical features of bacteraemia caused by different MAC species. In this study, the clinical characteristics of patients treated for MAC bacteraemia in...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2017.02.016
更新日期:2017-07-01 00:00:00
abstract::Gentamicin-containing polymethylmethacrylate (PMMA) beads are frequently used to prevent and treat orthopaedic infections. The beads are typically inserted to fill anatomical defects secondary to surgical debridement. Local gentamicin use results in low serum levels whilst achieving high concentrations at the site of ...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章,评审
doi:10.1016/j.ijantimicag.2011.03.008
更新日期:2011-11-01 00:00:00
abstract::New treatments are urgently required for infections caused by meticillin-resistant Staphylococcus aureus (MRSA) as these strains are often resistant to multiple conventional antibiotics. Earlier studies showed that ranalexin, an antimicrobial peptide (AMP), in combination with lysostaphin, an antistaphylococcal endope...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2010.01.016
更新日期:2010-06-01 00:00:00
abstract::For several years, the threat of antibiotic resistance and its health cost has dramatically risen and various alarming figures have been proposed to illustrate the mortality due to antibiotic resistance. However, predictions concerning different living beings are doomed to failure, as theorised in Alice's 'living croq...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章,评审
doi:10.1016/j.ijantimicag.2016.11.015
更新日期:2017-05-01 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::This review will summarise the relevant pathophysiology of sepsis, the rationale for treatment with recombinant human activated protein C and the evidence for and against its use, and will provide evidence-based recommendations for its administration. ...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章,评审
doi:10.1016/j.ijantimicag.2006.05.021
更新日期:2006-08-01 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::The objective of this study was to obtain data on the susceptibility of pathogens responsible for acute uncomplicated cystitis in South Korea to currently used antimicrobial agents. A total of 239 isolates were obtained from female outpatients with acute uncomplicated cystitis. The most prevalent causative organism wa...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章,多中心研究
doi:10.1016/j.ijantimicag.2004.02.012
更新日期:2004-09-01 00:00:00
abstract::The purpose of this report was to compare two different methods for dose optimisation of antimicrobials. The probability of target attainment (PTA) was calculated using Monte Carlo simulation to predict the PK/PD target of fT>MIC or modelling and simulation of time-kill curve data. Ceftobiprole, the paradigm compound,...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2013.08.016
更新日期:2014-01-01 00:00:00
abstract::The selection of antimicrobial agents is guided by the use of formularies which often constrain prescribing options. There are several factors which influence the inclusion of specific agents. Two of the most important factors are microbial etiology of a disease and the incidence of antibiotic resistance. Various surv...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/s0924-8579(98)00107-1
更新日期:1999-07-01 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::The in vitro activity of moxifloxacin was compared with that of penicillin G, amoxycillin/clavulanate, cefoxitin, erythromycin, clindamycin and metronidazole against 158 isolates associated with periodontal infections. MIC(50)/MIC(90) values of moxifloxacin were respectively 0.06/0.5 mg/l for Porphyromonas gingivalis ...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/s0924-8579(02)00190-5
更新日期:2002-12-01 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::Cystic fibrosis (CF) patients are at risk of acquiring chronic Pseudomonas aeruginosa lung infections. The biofilm mode of growth of P. aeruginosa induces tolerance to antibiotics and the host response; accordingly, treatment failure occurs. Supplemental azithromycin has proven beneficial in CF owing to potential immu...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2020.106213
更新日期:2021-01-01 00:00:00
abstract::Tigecycline, is a novel broad-spectrum glycylcycline antibiotic, which has activity against a broad range of Gram-positive, Gram-negative, atypical, anaerobic and antibiotic-resistant bacteria. This includes activity against MRSA, VRE and penicillin resistant Streptococcus pneumoniae. Whilst exhibiting antibacterial a...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章,评审
doi:10.1016/j.ijantimicag.2004.11.006
更新日期:2005-03-01 00:00:00
abstract::The in vitro activity of the steroidal amide 3beta-acetoxy-17beta-(L-prolyl)amino-5alpha-androstane against 179 gram-positive clinical isolates was examined. The minimum bactericidal concentration (MBC)/MIC ratios were < or = 2 for 73% of methicillin-resistant Staphyllococcus aureus, 59% of vancomycin-resistant Entero...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/s0924-8579(00)00156-4
更新日期:2000-08-01 00:00:00
abstract::This study investigated the correlation between fluoroquinolone (ciprofloxacin or levofloxacin) use and rates of fluoroquinolone resistance in Pseudomonas aeruginosa isolates from patients with nosocomial infection at a medical centre in Taiwan. Antibiotic utilisation data were extracted on a monthly basis from the in...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2009.11.007
更新日期:2010-03-01 00:00:00
abstract::We employed an in-vivo pharmacokinetic/in-vitro pharmacodynamic method to simulate bacterial killing in plasma and the interstitium of skeletal muscle tissue after intravenous administration of 2 g of cefpirome and 8 g of fosfomycin alone and in combination to patients with sepsis. Interstitial antimicrobial concentra...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/s0924-8579(03)00047-5
更新日期:2003-06-01 00:00:00
abstract::This study aimed to forecast the incidence rate of carbapenem resistance and to assess the impact of an antimicrobial stewardship intervention using routine antimicrobial consumption surveillance data. Following an outbreak of OXA-48-producing Klebsiella pneumoniae (January 2008-April 2010) in a renal cohort in London...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2015.03.005
更新日期:2015-08-01 00:00:00
abstract::Respiratory tract infections (RTIs) form a substantial clinical and financial burden, with the increasing complication of antimicrobial resistance. This resistance may compromise the use of many empirically prescribed antimicrobials. The new respiratory fluoroquinolones have been developed to overcome this burgeoning ...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章,评审
doi:10.1016/j.ijantimicag.2007.12.003
更新日期:2008-04-01 00:00:00
abstract::This study determined the etiology of lower respiratory tract infections in the elderly and assessed whether the growth of beta-lactamase producing bacteria is particularly favoured in these patients. Between December 1998 and May 1999, 187 patients with community-acquired pneumonia (CAP), and 887 patients with acute ...
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::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::Resistance to extended-spectrum β-lactams is increasing worldwide among Escherichia coli and has been linked to a small number of emergent clones (e.g. ST38, ST131 and ST405) recovered from extraintestinal infections in community and hospital settings. There are, however, limited data about the relative contributions ...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2013.01.006
更新日期:2013-05-01 00:00:00
abstract::A recent report identified significant reductions or disappearance of viral load in COVID-19 patients given a combination of hydroxychloroquine and azithromycin. The present communication discusses some common pharmacokinetic properties of these two drugs that may be linked to a potential underlying mechanism of actio...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2020.106007
更新日期:2020-06-01 00:00:00
abstract::Extended-spectrum β-lactamase-producing Escherichia coli (ESBL-Ec) is a frequent cause of acute pyelonephritis (APN), requiring carbapenem therapy. However, alternatives to carbapenems are needed due to the emergence of carbapenemase-producing micro-organisms. The purpose of this study was to compare the clinical effi...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2016.12.017
更新日期:2017-04-01 00:00:00