Abstract:
OBJECTIVES:Malaria treatment is impeded by increasing resistance to conventional antimalarial drugs. Here we explored the activity of ten novel benzothiophene, thiophene and benzene aminoquinolines. METHODS:In vitro testing was performed by the lactate dehydrogenase assay in chloroquine (CQ)-sensitive Plasmodium falciparum strain 3D7 and CQ-resistant (CQR) P. falciparum strain Dd2. In vivo activity was evaluated by a modified Thompson test using C57BL/6 mice infected with Plasmodium berghei ANKA strain. RESULTS:Nine of the ten compounds had a lower 50% inhibitory concentration (IC50) than CQ against the CQR strain Dd2. Five of these compounds that were available for in vivo evaluation were shown to be non-toxic. All five compounds administered at a dose of 160mg/kg/day for 3 days prolonged the survival of treated compared with untreated mice. Untreated control mice died by Day 7 with a mean parasitaemia of 15%. Among treated mice, a dichotomous outcome was observed, with a two-third majority of treated mice dying by Day 17 with a low mean parasitaemia of 5%, whilst one-third survived longer with a mean hyperparasitaemia of 70%; specifically, five of these mice survived a mean of 25 days, whilst two even survived past Day 31. CONCLUSIONS:The significant antimalarial potential of this aminoquinoline series is illustrated by its excellent in vitro activity against the CQRP. falciparum strain and significant in vivo activity. Interestingly, compounds ClAQ7, ClAQ9 and ClAQ11 were able to confer resistance to cerebral malaria and afford a switch to hyperparasitaemia to mice prone to the neurological syndrome.
journal_name
J Glob Antimicrob Resistjournal_title
Journal of global antimicrobial resistanceauthors
Srbljanović J,Bobić B,Štajner T,Uzelac A,Opsenica I,Terzić-Jovanović N,Bauman N,Šolaja BA,Djurković-Djaković Odoi
10.1016/j.jgar.2020.07.027subject
Has Abstractpub_date
2020-12-01 00:00:00pages
20-25eissn
2213-7165issn
2213-7173pii
S2213-7165(20)30202-2journal_volume
23pub_type
杂志文章abstract:OBJECTIVES:Klebsiella pneumoniae, which exists in the intestinal and respiratory tracts of humans and animals, is an important conditional pathogen in many animals. The aim of the current study was to investigate the antimicrobial resistance profiles and genotypes of extended-spectrum β-lactamase (ESBL)- and AmpC β-lac...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2017.06.006
更新日期:2017-09-01 00:00:00
abstract::Acinetobacter calcoaceticus-baumannii complex is a common cause of hospital-acquired infections (HAIs) globally, remarkable for its high rate of antibiotic resistance, including to carbapenems. There are few data on the resistance of A. baumannii in Vietnam, which are essential for developing evidence-based treatment ...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2014.05.003
更新日期:2014-12-01 00:00:00
abstract::Hospitals in Hong Kong, like many hospitals in the world, are constantly challenged by the increasing rate of non-susceptible and multidrug-resistant organisms (MDROs). Accurate and timely surveillance is essential for effective control. The Hospital Authority of Hong Kong has developed a comprehensive antimicrobial s...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章,评审
doi:10.1016/j.jgar.2014.05.008
更新日期:2014-12-01 00:00:00
abstract:OBJECTIVES:The aim of this study was to evaluate the role of residue 238 in CTX-M-15 and CTX-M-15G238C mutant with respect to carbapenems and various β-lactamase inhibitors. METHODS:A CTX-M-15G238C laboratory mutant was generated by site-directed mutagenesis from CTX-M-15 enzyme by replacing glycine 238 with cysteine....
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2017.04.004
更新日期:2017-09-01 00:00:00
abstract:BACKGROUND:OXA-48 is an Ambler class D β-lactamase that hydrolyses penicillin and imipenem but has poor hydrolytic activity against cephalosporins. However, very few clinical experiences of treating extended-spectrum β-lactamase (ESBL)-negative OXA-48 producers with cephalosporins have been published. OBJECTIVES:The a...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2019.02.016
更新日期:2019-12-01 00:00:00
abstract:OBJECTIVES:Ralstonia pickettii has been increasingly recognised as an emerging opportunistic pathogen in hospital settings in recent years, especially in patients with prolonged hospital stay. Clinical manifestations associated with R. pickettii infection range from mild infections to severe invasive life-threatening i...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2020.02.020
更新日期:2020-06-01 00:00:00
abstract:OBJECTIVES:Isoniazid (INH) resistance is a major contributor to the emergence of multidrug resistance in Mycobacterium tuberculosis (MTB), hampering the success of tuberculosis treatment. This study aimed to identify good leads based on INH derivatives against INH-resistant MTB strains. Mutations at codon 315 in the ka...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2017.06.014
更新日期:2017-12-01 00:00:00
abstract:OBJECTIVES:Here we describe a clinical isolate of Klebsiella pneumoniae ST11 harbouring both blaKPC-2 and rmtB genes in Japan. METHODS:A carbapenem- and aminoglycoside-resistant K. pneumoniae was isolated from an inpatient in Japan. Whole-genome sequencing (WGS) was performed using an Illumina next-generation sequence...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2018.11.026
更新日期:2019-06-01 00:00:00
abstract:OBJECTIVES:Infections caused by multidrug-resistant Gram-negative bacteria are associated with high mortality. A relevant concern is the efficacy of antibiotic therapy in burn patients in whom pathophysiological changes strongly influence pharmacokinetic (PK) parameters. This study aimed to describe the PK parameters o...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2019.06.011
更新日期:2020-03-01 00:00:00
abstract:OBJECTIVES:Staphylococcus aureus remains the most important cause of infections in hospitals and long-term care facilities. The aim of this study was to analyse the resistance, virulence, and epidemiological and genetic relationships of S. aureus from bloodstream infections (BSIs) and pneumonia from patients in Souther...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2017.07.009
更新日期:2017-12-01 00:00:00
abstract:OBJECTIVES:Rates of nosocomial infections caused by carbapenem-resistant Klebsiella pneumoniae (CRKP) have increased. A meta-analysis was conducted to explore risk factors for CRKP infection in order to provide a theoretical basis for reducing the CRKP infection rate and actively preventing CRKP infection. METHODS:Onl...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2019.09.006
更新日期:2020-06-01 00:00:00
abstract::The objective of this review was to describe the 'state of the art' of Plasmodium falciparum resistance to the main antimalarial drugs. A brief note on Plasmodium vivax is also included. Resistance of P. falciparum to the various antimalarials has a long history of hits and misses. During the last 60 years, the pace a...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章,评审
doi:10.1016/j.jgar.2015.02.002
更新日期:2015-06-01 00:00:00
abstract:OBJECTIVES:Biofilms associated with implantable medical devices and wounds are clinically relevant, often requiring repeated use of antibiotics without success. A search for non-antibiotic antimicrobial and antibiofilm solutions is warranted, in line with antimicrobial stewardship. Our study aimed to evaluate the broad...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2020.12.002
更新日期:2020-12-28 00:00:00
abstract:OBJECTIVES:The aim of this study was to explore the genomic content of a blaKPC-2- and mcr-1-harbouring Escherichia coli strain and to clarify the molecular mechanism for the transmission of multidrug resistance. METHODS:Antimicrobial susceptibility testing was conducted by the broth microdilution method to determine ...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2020.08.023
更新日期:2020-12-01 00:00:00
abstract::The two closely related mycobacteria, Mycobacterium intracellulare and Mycobacterium chimaera, exhibit a more than two-fold difference in their in vitro susceptibility to sulfonamides. Sulfonamides are antibiotics targeting the 6-hydroxymethyl-7,8-dihydropteroate synthase (DHPS) enzyme involved in the folate synthesis...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2013.05.003
更新日期:2013-12-01 00:00:00
abstract:OBJECTIVES:Acinetobacter spp. isolates carrying the blaNDM-1 gene are frequently reported. However, most reported blaNDM-1 genes are carried by clinical strains. Here we report a carbapenem-resistant Acinetobacter towneri isolate from hospital sewage in China co-harbouring blaNDM-1 and blaOXA-58 in the genome. METHODS...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2018.11.015
更新日期:2019-03-01 00:00:00
abstract::Various molecular methods have been developed to rapidly detect clarithromycin (CLR) resistance in Helicobacter pylori isolates in clinical specimens. All of these assays for detecting CLR resistance in H. pylori are based on detection of mutations in the 23S rRNA gene. In this article, we summarise current knowledge ...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章,评审
doi:10.1016/j.jgar.2016.01.002
更新日期:2016-03-01 00:00:00
abstract::Environmental fungicides are used in agriculture to reduce fungal spoilage of crops to a minimum, and the polyene macrolide natamycin is used as a food preservative. The use of natamycin in yoghurt has recently been authorised in the USA and some other countries. However, resistance development is a serious risk assoc...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章,评审
doi:10.1016/j.jgar.2017.10.024
更新日期:2018-06-01 00:00:00
abstract:OBJECTIVES:The aim of this study was to forecast the monthly incidence rates of infections [infections/1000 bed-days (IBD)] due to carbapenem-resistant Klebsiella pneumoniae (CRKP), carbapenem-resistant Pseudomonas aeruginosa (CRPA), carbapenem-resistant Acinetobacter baumannii (CRAB) and total carbapenem-resistant Gra...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2019.06.019
更新日期:2020-03-01 00:00:00
abstract:OBJECTIVES:Thousands of cases of multidrug-resistant tuberculosis (TB) have been observed in the Philippines, but studies on the Mycobacterium tuberculosis (MTB) genotypes that underlie the observed drug resistance profiles are lacking. This study aimed to analyse the whole genomes of clinical MTB isolates representing...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2018.08.009
更新日期:2018-12-01 00:00:00
abstract:OBJECTIVES:Mortality associated with carbapenemase-producing Enterobacteriaceae is high as there are few therapeutic options. Escherichia coli sequence type 410 (ST410) is currently an international high-risk clone and is responsible for a large number of clinical infections. Here we report the draft genome sequence of...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2019.10.027
更新日期:2019-12-01 00:00:00
abstract:OBJECTIVES:Multidrug-resistant (MDR) enterococci are found extensively in food samples. This study characterized the phenotypic virulence factors and the ability of horizontal gene transfer of a streptomycin resistance gene among enterococci isolated from fermented pork. METHODS:Thirty-six MDR enterococci were subject...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2020.04.016
更新日期:2020-09-01 00:00:00
abstract:OBJECTIVES:Limited data have been reported regarding osteomyelitis due to carbapenemase-producing Enterobacteriaceae (CPE), including co-infections with extended-spectrum β-lactamase (ESBL)-producing micro-organisms. METHODS:We conducted a retrospective study in a reference centre for bone and joint infections from 20...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2020.08.007
更新日期:2020-12-01 00:00:00
abstract:OBJECTIVES:The aim of study was to evaluate by comparative study the level of selection of antibiotic-resistant Enterobacteriaceae in the digestive microbiota of piglets when using amoxicillin and Algo-Bio®. METHODS:Amoxicillin and Algo-Bio® administration was carried out over a period of 5 days (D0-D4) at a dose of 1...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2018.01.008
更新日期:2018-06-01 00:00:00
abstract:BACKGROUND AND AIM:The global rise of antimicrobial resistance among bacterial strains is a rapidly growing challenge and is becoming a major public health concern. This study documents the worldwide spread and genotype distribution of human clinical isolates of New Delhi metallo-β-lactamase-producing Klebsiella pneumo...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章,评审
doi:10.1016/j.jgar.2020.10.016
更新日期:2020-12-01 00:00:00
abstract:OBJECTIVES:The aim of this study was to evaluate the efficacy of pyrimethamine-loaded poloxamer 407 nanomicelles on Plasmodium berghei strain NICD in vivo. METHODS:Pyrimethamine-loaded nanomicelles were prepared and their zeta potential, particle size and polydispersity index were measured. For antiplasmodial assessme...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2019.08.002
更新日期:2020-03-01 00:00:00
abstract:OBJECTIVES:Vancomycin is the primary treatment for methicillin-resistant Staphylococcus aureus (MRSA). However, an increasing proportion of MRSA isolates with high minimum inhibitory concentrations (MICs) within the susceptible range (vancomycin 'MIC creep') is being observed. The aim of this study was to assess the va...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2017.04.007
更新日期:2017-09-01 00:00:00
abstract::Antimicrobial resistance severely limits the therapeutic options for many clinically important bacteria. In Gram-negative bacteria, multidrug resistance is commonly facilitated by plasmids that have the ability to accumulate and transfer refractory genes amongst bacterial populations. The aim of this study was to isol...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2016.01.011
更新日期:2016-06-01 00:00:00
abstract:OBJECTIVES:This study aimed to characterise insertional mutations disturbing themgrB gene in carbapenem-resistant Klebsiella pneumoniae (CRKp). METHODS:A total of 118 clinical CRKp isolates were surveyed for polymyxin resistance and insertion sequence (IS) elements disruptingmgrB. RESULTS:Of the 118 isolates, 78 (66....
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2020.11.003
更新日期:2020-11-24 00:00:00
abstract:OBJECTIVES:Cutibacterium acnes (formerly Propionibacterium acnes), an anaerobic Gram-positive bacterium, is a skin commensal and is considered to be associated with acne. Here we report the draft genome sequences of three multidrug-resistant (MDR) C. acnes strains (CA17, CA39 and CA51) isolated from skin lesions of acn...
journal_title:Journal of global antimicrobial resistance
pub_type: 杂志文章
doi:10.1016/j.jgar.2017.10.008
更新日期:2017-12-01 00:00:00