Two 2-hydroxy-3-alkyl-1,4-naphthoquinones with in vitro and in vivo activities against Toxoplasma gondii.

Abstract:

:Two 3-alkyl-substituted 2-hydroxy-1,4-naphthoquinones, NSC 113452 (NSC52) and NSC 113455 (NSC55), were evaluated for activity against Toxoplasma gondii in vitro and in murine models of acute toxoplasmosis. In vitro, both NSC52 and NSC55 significantly inhibited intracellular replication of T. gondii. In vivo, each compound was examined alone and in combination with other drugs currently used for treatment of human toxoplasmosis. Although none of the compounds protected mice against death when administered orally, both were significantly protective when administered intraperitoneally. In addition, a significant increase in survival was observed when suboptimal doses of each compound were used in combination with suboptimal doses of pyrimethamine or sulfadiazine. These results indicate that combinations of NSC52 or NSC55 with pyrimethamine or sulfadiazine have promising activity against T. gondii.

authors

Khan AA,Nasr M,Araujo FG

doi

10.1128/AAC.42.9.2284

subject

Has Abstract

pub_date

1998-09-01 00:00:00

pages

2284-9

issue

9

eissn

0066-4804

issn

1098-6596

journal_volume

42

pub_type

杂志文章
  • Elimination of plasmid pMG110 from Escherichia coli by novobiocin and other inhibitors of DNA gyrase.

    abstract::The ability of novobiocin to eliminate (cure) the wild-type plasmid pMG110 from Escherichia coli has been compared with that of other inhibitors of the gyrase B subunit and of the gyrase A subunit. Novobiocin eliminated pMG110 , producing over 99% plasmid loss at concentrations two- to eightfold below the MIC for bact...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.25.5.586

    authors: Hooper DC,Wolfson JS,McHugh GL,Swartz MD,Tung C,Swartz MN

    更新日期:1984-05-01 00:00:00

  • Successful Systemic and Topical Treatment of Mycobacterium abscessus Otomastoiditis.

    abstract::Mycobacterium abscessus is an extensively drug-resistant opportunistic pathogen that can cause chronic otomastoiditis. There are no evidence-based treatment regimens for this severe infection. We treated four children with M. abscessus otomastoiditis with a structured regimen of topical imipenem and tigecycline, intra...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01203-19

    authors: van Wijk F,Waterval J,van Aerde K,Henriet SSV,Meijer FJA,Borra LC,Aarnoutse RE,van Ingen J

    更新日期:2019-12-20 00:00:00

  • Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.

    abstract::The objective of this study was to determine the population pharmacokinetic parameters of levofloxacin, gatifloxacin, and moxifloxacin following multiple oral doses. Twenty-nine patients with tuberculosis at the University Hospital in Vitória, Brazil, participated. Subjects received multiple doses of one drug (levoflo...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,随机对照试验

    doi:10.1128/AAC.01036-07

    authors: Peloquin CA,Hadad DJ,Molino LP,Palaci M,Boom WH,Dietze R,Johnson JL

    更新日期:2008-03-01 00:00:00

  • Enhancement of drug susceptibility in Plasmodium falciparum in vitro and Plasmodium berghei in vivo by mixed-function oxidase inhibitors.

    abstract::A number of compounds, as exemplified by verapamil and desipramine, have been shown to enhance the susceptibility of resistant malaria parasites to chloroquine. The mechanism by which these agents reverse resistance is still controversial but is though to involve alterations in drug transport causing an increase in st...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.37.6.1318

    authors: Ndifor AM,Howells RE,Bray PG,Ngu JL,Ward SA

    更新日期:1993-06-01 00:00:00

  • Efficacy of amphotericin B or itraconazole in a murine model of central nervous system Aspergillus infection.

    abstract::Given the greater than 90% lethality of clinical central nervous system (CNS) aspergillosis despite current therapies, there is a need for an animal model to study therapeutic strategies. We previously established a model of CNS aspergillosis by intracerebral infection and report here the results of treatment with the...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.2.813-815.2003

    authors: Chiller TM,Sobel RA,Luque JC,Clemons KV,Stevens DA

    更新日期:2003-02-01 00:00:00

  • Effect of amphotericin B and rifampin against Coccidioides immitis in vitro and in vivo.

    abstract::Amphotericin B, the principal drug used for treating systemic mycoses, possesses undesirable toxic properties. The ability of this antibiotic to potentiate antifungal activity of other compounds suggests that lower doses of amphotericin B could be used in combination with a second drug without loss of therapeutic effi...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.9.3.406

    authors: Huppert M,Pappagianis D,Sun SH,Gleason-Jordan I,Collins MS,Vukovich KR

    更新日期:1976-03-01 00:00:00

  • LfrR is a repressor that regulates expression of the efflux pump LfrA in Mycobacterium smegmatis.

    abstract::The lfrA gene of Mycobacterium smegmatis encodes an efflux pump which mediates resistance to different fluoroquinolones, cationic dyes, and anthracyclines. The deletion of the lfrR gene, coding for a putative repressor and localized upstream of lfrA, increased the lfrA expression. In this study, reverse transcription-...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00656-06

    authors: Buroni S,Manina G,Guglierame P,Pasca MR,Riccardi G,De Rossi E

    更新日期:2006-12-01 00:00:00

  • In vitro intracellular activity and in vivo efficacy of modithromycin, a novel bicyclolide, against Legionella pneumophila.

    abstract::The in vitro and in vivo activities of modithromycin, a novel bicyclolide, against Legionella pneumophila were compared with those of telithromycin, clarithromycin, azithromycin, and levofloxacin. All the test agents decreased the intracellular growth of viable L. pneumophila bacteria over 96 h of incubation in both t...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01474-10

    authors: Sato T,Tateda K,Kimura S,Ishii Y,Yamaguchi K

    更新日期:2011-04-01 00:00:00

  • Identification of a Novel Gene Associated with High-Level β-Lactam Resistance in Heterogeneous Vancomycin-Intermediate Staphylococcus aureus Strain Mu3 and Methicillin-Resistant S. aureus Strain N315.

    abstract::β-Lactam resistance levels vary among methicillin-resistant Staphylococcus aureus (MRSA) clinical isolates, mediated by chromosomal mutations and exogenous resistance gene mecA However, MRSA resistance mechanisms are incompletely understood. A P440L mutation in the RNA polymerase β' subunit (RpoC) in slow-vancomycin-i...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00712-18

    authors: Matsuo M,Yamamoto N,Hishinuma T,Hiramatsu K

    更新日期:2019-01-29 00:00:00

  • In Vitro Synergy and In Vivo Activity of Tigecycline-Ciprofloxacin Combination Therapy against Vibrio vulnificus Sepsis.

    abstract::The mortality rate associated with Vibrio vulnificus sepsis remains high. An in vitro time-kill assay revealed synergism between tigecycline and ciprofloxacin. The survival rate was significantly higher in mice treated with tigecycline plus ciprofloxacin than in mice treated with cefotaxime plus minocycline. Thus, com...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00310-19

    authors: Kim SE,Kim HK,Choi SM,Yu Y,Kim UJ,Darboe KS,Kang SJ,Park KH,Kang G,Kim YR,Rhee JH,Jung SI,Jang HC

    更新日期:2019-09-23 00:00:00

  • Complete nucleotide sequences of bla(CTX-M)-harboring IncF plasmids from community-associated Escherichia coli strains in the United States.

    abstract::Community-associated infections due to Escherichia coli producing CTX-M-type extended-spectrum β-lactamases are increasingly recognized in the United States. The bla(CTX-M) genes are frequently carried on IncF group plasmids. In this study, bla(CTX-M-15)-harboring plasmids pCA14 (sequence type 131 [ST131]) and pCA28 (...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.04772-14

    authors: Li JJ,Spychala CN,Hu F,Sheng JF,Doi Y

    更新日期:2015-01-01 00:00:00

  • Effects of a high-fat meal on the relative oral bioavailability of piperaquine.

    abstract::Piperaquine (PQ) is an antimalarial drug whose high lipid solubility suggests that its absorption can be increased by a high-fat meal. We examined the pharmacokinetics of PQ phosphate (500 mg given orally) in the fasting state and after a high-fat meal in eight healthy Caucasian volunteers (randomized crossover). Plas...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1128/AAC.49.6.2407-2411.2005

    authors: Sim IK,Davis TM,Ilett KF

    更新日期:2005-06-01 00:00:00

  • Mycobacterium tuberculosis embB codon 306 mutations confer moderately increased resistance to ethambutol in vitro and in vivo.

    abstract::Ethambutol (EMB) is a major component of the first-line therapy of tuberculosis. Mutations in codon 306 of embB (embB306) were suggested as a major resistance mechanism in clinical isolates. To directly analyze the impact of individual embB306 mutations on EMB resistance, we used allelic exchange experiments to genera...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00007-10

    authors: Plinke C,Walter K,Aly S,Ehlers S,Niemann S

    更新日期:2011-06-01 00:00:00

  • Ceftriaxone pharmacokinetics in patients with various degrees of renal impairment.

    abstract::The effects of renal impairment on the pharmacokinetics of ceftriaxone in humans were examined after intravenous infusion of a 1-g dose over 15 min to 30 renally impaired patients. The study included 12 dialysis patients and 18 patients with severe, moderate, or mild renal impairment. Plasma and, where appropriate, ur...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.25.4.438

    authors: Patel IH,Sugihara JG,Weinfeld RE,Wong EG,Siemsen AW,Berman SJ

    更新日期:1984-04-01 00:00:00

  • Different genetic supports for the tet(S) gene in Enterococci.

    abstract::The diversity of tet(S) genetic contexts of 13 enterococci from human, animal, and environmental samples from different geographical areas is reported. The tet(S) gene was linked to either CTn6000 variants of chromosomal location or composite platforms flanked by IS1216 located on plasmids (∼40 to 115 kb). The compara...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00758-12

    authors: Novais C,Freitas AR,Silveira E,Baquero F,Peixe L,Roberts AP,Coque TM

    更新日期:2012-11-01 00:00:00

  • Synergistic activity of colistin and ceftazidime against multiantibiotic-resistant Pseudomonas aeruginosa in an in vitro pharmacodynamic model.

    abstract::Despite the marketing of a series of new antibiotics for antibiotic-resistant gram-positive bacteria, no new agents for multiple-antibiotic-resistant gram-negative infections will be available for quite some time. Clinicians will need to find more effective ways to utilize available agents. Colistin is an older but no...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.3.905-909.2003

    authors: Gunderson BW,Ibrahim KH,Hovde LB,Fromm TL,Reed MD,Rotschafer JC

    更新日期:2003-03-01 00:00:00

  • Treatment of encrusted cystitis caused by Corynebacterium group D2 with norfloxacin, ciprofloxacin, and teicoplanin in an experimental model in rats.

    abstract::Oral doses of norfloxacin (80 mg/kg of body weight per day) and ciprofloxacin (25 and 80 mg/kg/day) and intramuscular doses of teicoplanin (5 mg/kg/day), all administered once a day for 10 days, were evaluated as a means of preventing encrusted cystitis caused by Corynebacterium group D2. Zinc disks dipped into a 24-h...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.35.12.2587

    authors: Soriano F,Rodriguez-Tudela JL,Castilla C,Avilés P

    更新日期:1991-12-01 00:00:00

  • Exudate levels and bactericidal activity of cefazolin in a new local infection system using rat granuloma pouches.

    abstract::An experimental local infection system has been developed in which exudates are induced with croton oil in granuloma pouches of rats. This system provided a suitable model for the evaluation of the therapeutic effect of two antibiotics, cefazolin and cephalothin. Exudate levels of cefazolin were found to be higher tha...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.11.6.1042

    authors: Nishida M,Murakawa T

    更新日期:1977-06-01 00:00:00

  • Saccharomicins, novel heptadecaglycoside antibiotics produced by Saccharothrix espanaensis: antibacterial and mechanistic activities.

    abstract::Saccharomicins A and B, two new heptadecaglycoside antibiotics, were isolated from the fermentation broth of the rare actinomycete Saccharothrix espanaensis. They represent a novel class of bactericidal antibiotics that are active both in vitro and in vivo against bacteria and yeast (MICs: Staphylococcus aureus, <0.12...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.44.8.2154-2159.2000

    authors: Singh MP,Petersen PJ,Weiss WJ,Kong F,Greenstein M

    更新日期:2000-08-01 00:00:00

  • Antileishmanial and antitrypanosomal activities of the 8-aminoquinoline tafenoquine.

    abstract::The 8-aminoquinoline tafenoquine showed significant in vitro activity against Leishmania species, including L. donovani amastigotes in macrophages, with 50% inhibitory concentrations (IC(50)s) between 0.1 and 4.0 μM for both pentavalent antimony (SbV)-sensitive and SbV-resistant strains and by oral administration in B...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00985-10

    authors: Yardley V,Gamarro F,Croft SL

    更新日期:2010-12-01 00:00:00

  • Efficacy and Safety of Pyronaridine-Artesunate plus Single-Dose Primaquine for Treatment of Uncomplicated Plasmodium falciparum Malaria in Eastern Cambodia.

    abstract::In Cambodia, multidrug-resistant Plasmodium falciparum undermines the treatment of uncomplicated malaria, and new therapeutic options are needed. Pyronaridine-artesunate has not previously been evaluated in eastern Cambodia. We conducted a single-arm, open-label, prospective study between July and December 2017 at the...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02242-18

    authors: Leang R,Mairet-Khedim M,Chea H,Huy R,Khim N,Mey Bouth D,Dorina Bustos M,Ringwald P,Witkowski B

    更新日期:2019-02-26 00:00:00

  • ICESp1116, the genetic element responsible for erm(B)-mediated, inducible resistance to erythromycin in Streptococcus pyogenes.

    abstract::ICESp1116, responsible for erm(B)-mediated, inducible erythromycin resistance in Streptococcus pyogenes, was comprehensively characterized, and its chromosomal integration site was determined. It displayed a unique mosaic organization consisting of a scaffold, related to TnGallo1 from Streptococcus gallolyticus, with ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01494-12

    authors: Brenciani A,Tiberi E,Morici E,Oryasin E,Giovanetti E,Varaldo PE

    更新日期:2012-12-01 00:00:00

  • Resistance gene transfer during treatments for experimental avian colibacillosis.

    abstract::An experiment was conducted in animal facilities to compare the impacts of four avian colibacillosis treatments-oxytetracycline (OTC), trimethoprim-sulfadimethoxine (SXT), amoxicillin (AMX), or enrofloxacin (ENR)-on the susceptibility of Escherichia coli in broiler intestinal tracts. Birds were first orally inoculated...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.05617-11

    authors: Dheilly A,Le Devendec L,Mourand G,Bouder A,Jouy E,Kempf I

    更新日期:2012-01-01 00:00:00

  • In vitro activity of LY146032 against staphylococci, streptococci, and enterococci.

    abstract::The in vitro activities of LY146032 and seven comparative antimicrobial agents against 14 species of staphylococci, streptococci, and enterococci were studied. MICs of LY146032 were less than or equal to 0.5 microgram/ml for all staphylococci, including oxacillin-resistant strains; less than or equal to 0.25 microgram...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.30.5.781

    authors: Fass RJ,Helsel VL

    更新日期:1986-11-01 00:00:00

  • Exploring ubiquinone biosynthesis inhibition as a strategy for improving atovaquone efficacy in malaria.

    abstract::Atovaquone (AV) acts on the malaria parasite by competing with ubiquinol (UQH2) for its union to the mitochondrial bc1 complex, preventing the ubiquinone-8,9 (UQ) redox recycling, which is a necessary step in pyrimidine biosynthesis. This study focused on UQ biosynthesis in Plasmodium falciparum and adopted proof-of-c...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01516-20

    authors: Verdaguer IB,Crispim M,Zafra CA,Sussmann RAC,Buriticá NL,Melo HR,Azevedo MF,Almeida FG,Kimura EA,Katzin AM

    更新日期:2021-01-25 00:00:00

  • Use of a new mouse model of Acinetobacter baumannii pneumonia to evaluate the postantibiotic effect of imipenem.

    abstract::Acinetobacter baumannii is responsible for severe nosocomial pneumonia. To evaluate new therapeutic regimens for infections due to multiresistant strains and to study the pharmacodynamic properties of various antibiotics, we developed an experimental mouse model of acute A. baumannii pneumonia. C3H/HeN mice rendered t...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.41.2.345

    authors: Joly-Guillou ML,Wolff M,Pocidalo JJ,Walker F,Carbon C

    更新日期:1997-02-01 00:00:00

  • Comparative susceptibilities of 173 aerobic and anaerobic bite wound isolates to sparfloxacin, temafloxacin, clarithromycin, and older agents.

    abstract::The in vitro activities of sparfloxacin, temafloxacin, ciprofloxacin, ofloxacin, clarithromycin, erythromycin, tetracycline, cephalothin, penicillin G, and amoxicillin-clavulanic acid against 173 recent clinical bite wound isolates were determined by agar dilution. Sparfloxacin was active against all strains (MIC for ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.37.5.1150

    authors: Goldstein EJ,Citron DM

    更新日期:1993-05-01 00:00:00

  • Comparative in vitro activities of DU-6859a, levofloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against 387 aerobic and anaerobic bite wound isolates.

    abstract::The activities of DU-6859a, levofloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against bite wound isolates were determined by the agar dilution method. DU-6859a was the most active compound (MICs, < or = 0.125 microg/ml) against all Pasteurella species, Staphylococcus aureus, and streptococci; anaerobes were sus...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.41.5.1193

    authors: Goldstein EJ,Citron DM,Hunt Gerardo S,Hudspeth M,Merriam CV

    更新日期:1997-05-01 00:00:00

  • Moxalactam in the therapy of serious infections.

    abstract::Sixty-seven patients were treated with moxalactam in a noncomparative trial of hospitalized patients; 32 had endometritis or chorioamnionitis, 12 had skin and soft tissue infections, 5 had osteomyelitis, 5 had pneumonia, 5 had urinary tract infections, 4 had arthritis, 2 had sepsis from an unknown source, 1 had endoca...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.21.4.650

    authors: Marier RL,Faro S,Sanders CV,Williams W,Derks F,Janney A,Aldridge K

    更新日期:1982-04-01 00:00:00

  • In vitro susceptibility testing methods for caspofungin against Aspergillus and Fusarium isolates.

    abstract::We investigated the relevance of prominent reduction in turbidity macroscopically (MIC) and formation of aberrant hyphal tips microscopically (minimum effective concentration; MEC) in measuring the in vitro activity of caspofungin against Aspergillus and Fusarium. Caspofungin generated low MICs and MECs against Asperg...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.45.1.327-330.2001

    authors: Arikan S,Lozano-Chiu M,Paetznick V,Rex JH

    更新日期:2001-01-01 00:00:00