Antibacterial activity of RU44790, a new N-tetrazolyl monocyclic beta-lactam.

Abstract:

:RU44790 belongs to a new class of synthetic monocyclic beta-lactam antibiotics which feature a bioisosteric tetrazole moiety instead of the more classical acidic functions at the N-1 position of the beta-lactam ring. Its antibacterial activity was evaluated against some 900 strains and was compared with those of other recent beta-lactam derivatives, especially aztreonam. RU44790 is endowed with potent activity against gram-negative bacteria. At less than or equal to 0.6 micrograms/ml, RU44790 inhibited 90% of all strains of the family Enterobacteriaceae with the exception of Citrobacter spp. (MIC for 90% of strains tested, 1.2 micrograms/ml). The activity was similar to that of aztreonam against strains that are normally susceptible to expanded-spectrum cephalosporins. On the other hand, the new compound was 10 to 100 times more potent than aztreonam and most of the other antibiotics tested against enterobacteria that produce chromosome-encoded or plasmid-mediated extended-spectrum beta-lactamases. Pseudomonas aeruginosa isolates were equally susceptible to both monobactams. RU44790 was inactive against staphylococci and had only marginal activity against streptococci (MIC for 50% of strains tested, 2.5 micrograms/ml). RU44790 was highly resistant to hydrolysis by various beta-lactamases, particularly cephalosporinases such as P99. The latter enzyme was also inhibited by the compound. RU44790 showed a high affinity for penicillin-binding protein 3 of Escherichia coli. The results suggest that RU44790 has good potential in the treatment of infections caused by gram-negative microorganisms.

authors

Chantot JF,Klich M,Teutsch G,Bryskier A,Collette P,Markus A,Seibert G

doi

10.1128/aac.36.8.1756

subject

Has Abstract

pub_date

1992-08-01 00:00:00

pages

1756-63

issue

8

eissn

0066-4804

issn

1098-6596

journal_volume

36

pub_type

杂志文章
  • Population pharmacokinetic-pharmacodynamic analysis of voriconazole and anidulafungin in adult patients with invasive aspergillosis.

    abstract::To evaluate the exposure-response relationships for efficacy and safety of voriconazole and anidulafungin in adult patients with invasive aspergillosis (IA), a population pharmacokinetic-pharmacodynamic (PK-PD) analysis was performed with data from a phase 3, prospective, double-blind, comparative study evaluating vor...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02809-13

    authors: Liu P,Mould DR

    更新日期:2014-08-01 00:00:00

  • Impact of low-level resistance to fluoroquinolones due to qnrA1 and qnrS1 genes or a gyrA mutation on ciprofloxacin bactericidal activity in a murine model of Escherichia coli urinary tract infection.

    abstract::We investigated the impact of low-level resistance to fluoroquinolones on the bactericidal activity of ciprofloxacin in a murine model of urinary tract infection. The susceptible Escherichia coli strain CFT073 (ciprofloxacin MIC [CIP MIC] of 0.008 microg/ml) was compared to its transconjugants harboring qnrA1 or qnrS1...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01664-08

    authors: Allou N,Cambau E,Massias L,Chau F,Fantin B

    更新日期:2009-10-01 00:00:00

  • In vitro and in vivo pharmacokinetics-pharmacodynamics of GV143253A, a novel trinem.

    abstract::The aim of the present study was to characterize the pharmacokinetic-pharmacodynamic relationship of GV143253A, a novel trinem anti-methicillin-resistant Staphylococcus aureus (MRSA) agent active against gram-positive cocci, including multidrug-resistant clinical isolates. An in vitro pharmacodynamic study with methic...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.2.770-776.2003

    authors: Ferrari L,Iavarone L,Braggio S,Di Modugno E

    更新日期:2003-02-01 00:00:00

  • Lysostaphin-coated catheters eradicate Staphylococccus aureus challenge and block surface colonization.

    abstract::Lysostaphin is an endopeptidase that kills Staphylococcus aureus, a predominant organism in catheter-related infections. Lysostaphin-coated catheters prevented catheter colonization by several strains of S. aureus, and activity was maintained for at least 4 days. Prophylactic use of lysostaphin in catheters may help p...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.48.7.2704-2707.2004

    authors: Shah A,Mond J,Walsh S

    更新日期:2004-07-01 00:00:00

  • Mutations conferring resistance to a potent hepatitis C virus serine protease inhibitor in vitro.

    abstract::BILN 2061 is a novel, specific hepatitis C virus (HCV) NS3 serine protease inhibitor discovered by Boehringer Ingelheim that has shown potent activity against HCV replicons in tissue culture and is currently under clinical investigation for the treatment of HCV infection. The poor fidelity of the HCV RNA-dependent RNA...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.48.6.2260-2266.2004

    authors: Lu L,Pilot-Matias TJ,Stewart KD,Randolph JT,Pithawalla R,He W,Huang PP,Klein LL,Mo H,Molla A

    更新日期:2004-06-01 00:00:00

  • Uptake of antibiotics by human polymorphonuclear leukocyte cytoplasts.

    abstract::Enucleated human polymorphonuclear leukocytes (PMN cytoplasts), which have no nuclei and only a few granules, retain many of the functions of intact neutrophils. To better define the mechanisms and intracellular sites of antimicrobial agent accumulation in human neutrophils, we studied the antibiotic uptake process in...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.34.6.1189

    authors: Hand WL,King-Thompson NL

    更新日期:1990-06-01 00:00:00

  • Molecular cloning, sequence analysis, and heterologous expression of the phosphinothricin tripeptide biosynthetic gene cluster from Streptomyces viridochromogenes DSM 40736.

    abstract::A fosmid library from genomic DNA of Streptomyces viridochromogenes DSM 40736 was constructed and screened for the presence of genes known to be involved in the biosynthesis of phosphinothricin tripeptide (PTT). Eight positives were identified, one of which was able to confer PTT biosynthetic capability upon Streptomy...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.49.1.230-240.2005

    authors: Blodgett JA,Zhang JK,Metcalf WW

    更新日期:2005-01-01 00:00:00

  • Treatment of bacterial meningitis with ceftizoxime.

    abstract::Ceftizoxime was evaluated in the treatment of 18 patients (6 adults and 12 children) with bacterial meningitis. In seven patients Haemophilus influenzae was the causative agent, in three Neisseria meningitidis, in five Streptococcus pneumoniae, and in one each alpha-streptococcus and Escherichia coli; one case was cul...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.25.2.258

    authors: Overturf GD,Cable DC,Forthal DN,Shikuma C

    更新日期:1984-02-01 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

  • Liquid chromatographic assay of ketoconazole.

    abstract::A reverse-phase, high-pressure liquid chromatographic method for the rapid and quantitative determination of ketoconazole has been developed. Drug levels from 0.5 to 10 microgram/ml can be determined in either yeast nitrogen base medium or human serum by using an octadecylsilane column. A retention time of 4.9 +/- 0.1...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.19.1.110

    authors: Andrews FA,Peterson LR,Beggs WH,Crankshaw D,Sarosi GA

    更新日期:1981-01-01 00:00:00

  • Hydrogenosome metabolism is the key target for antiparasitic activity of resveratrol against Trichomonas vaginalis.

    abstract::Metronidazole (MDZ) and related 5-nitroimidazoles are the recommended drugs for treatment of trichomoniasis, a sexually transmitted disease caused by the protozoan parasite Trichomonas vaginalis. However, novel treatment options are needed, as recent reports have claimed resistance to these drugs in T. vaginalis isola...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00009-13

    authors: Mallo N,Lamas J,Leiro JM

    更新日期:2013-06-01 00:00:00

  • Renal glycosuria as a novel early sign of colistin-induced kidney damage in mice.

    abstract::The polymixin colistin represents a last resort antibiotic for multidrug resistant infections, but its use is limited by the frequent onset of acute drug-induced kidney injury (DIKI). It is essential to closely monitor kidney function prior to and during colistin treatment in order to pinpoint early signs of injury an...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01650-19

    authors: Samodelov SL,Visentin M,Gai Z,Häusler S,Kullak-Ublick GA

    更新日期:2019-10-07 00:00:00

  • N-acylated derivatives of sulfamethoxazole and sulfafurazole inhibit intracellular growth of Chlamydia trachomatis.

    abstract::Antibacterial compounds with novel modes of action are needed for management of bacterial infections. Here we describe a high-content screen of 9,800 compounds identifying acylated sulfonamides as novel growth inhibitors of the sexually transmitted pathogen Chlamydia trachomatis. The effect was bactericidal and distin...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02015-13

    authors: Marwaha S,Uvell H,Salin O,Lindgren AE,Silver J,Elofsson M,Gylfe A

    更新日期:2014-05-01 00:00:00

  • Burkholderia pseudomallei class a beta-lactamase mutations that confer selective resistance against ceftazidime or clavulanic acid inhibition.

    abstract::Burkholderia pseudomallei, the causative agent of melioidosis, is inherently resistant to a variety of antibiotics including aminoglycosides, macrolides, polymyxins, and beta-lactam antibiotics. Despite resistance to many beta-lactams, ceftazidime and beta-lactamase inhibitor-beta-lactam combinations are commonly used...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.7.2082-2087.2003

    authors: Tribuddharat C,Moore RA,Baker P,Woods DE

    更新日期:2003-07-01 00:00:00

  • In vitro and in vivo activity of LY 146032, a new cyclic lipopeptide antibiotic.

    abstract::The in vitro activity of LY 146032, a cyclic lipopeptide antibiotic belonging to the class of agents designated A21978C, was compared with those of vancomycin, cefpirome, cefotaxime, and clindamycin against selected gram-positive bacteria. The new drug inhibited all staphylococcal isolates, including methicillin-resis...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.30.4.532

    authors: Eliopoulos GM,Willey S,Reiszner E,Spitzer PG,Caputo G,Moellering RC Jr

    更新日期:1986-10-01 00:00:00

  • Novel Ser79Leu and Ser81Ile substitutions in the quinolone resistance-determining regions of ParC topoisomerase IV and GyrA DNA gyrase subunits from recent fluoroquinolone-resistant Streptococcus pneumoniae clinical isolates.

    abstract::Resistance of Streptococcus pneumoniae to fluoroquinolones is caused predominantly by amino acid substitutions at positions Ser79 of ParC and Ser81 of GyrA to either Phe or Tyr encoded in the quinolone resistance-determining regions of the parC topoisomerase IV and gyrA DNA gyrase genes. Analysis of highly resistant c...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.49.6.2479-2486.2005

    authors: Korzheva N,Davies TA,Goldschmidt R

    更新日期:2005-06-01 00:00:00

  • Effects of flavophospholipol on resistance in fecal Escherichia coli and enterococci of fattening pigs.

    abstract::A "plasmid-curing effect" of multiresistant Escherichia coli by flavophospholipol, an antibiotic used as an antimicrobial growth promoter (AMGP) in animal feeds, has been reported to occur in vitro and in vivo under experimental conditions. In this study, the effect of flavophospholipol under field conditions was stud...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.46.1.110-118.2002

    authors: van den Bogaard AE,Hazen M,Hoyer M,Oostenbach P,Stobberingh EE

    更新日期:2002-01-01 00:00:00

  • Bis-acridines as lead antiparasitic agents: structure-activity analysis of a discrete compound library in vitro.

    abstract::Parasitic diseases are of enormous public health significance in developing countries-a situation compounded by the toxicity of and resistance to many current chemotherapeutics. We investigated a focused library of 18 structurally diverse bis-acridine compounds for in vitro bioactivity against seven protozoan and one ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01418-06

    authors: Caffrey CR,Steverding D,Swenerton RK,Kelly B,Walshe D,Debnath A,Zhou YM,Doyle PS,Fafarman AT,Zorn JA,Land KM,Beauchene J,Schreiber K,Moll H,Ponte-Sucre A,Schirmeister T,Saravanamuthu A,Fairlamb AH,Cohen FE,McKerrow

    更新日期:2007-06-01 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

  • Cellular uptake and biological effects of antisense oligodeoxynucleotide analogs targeted to herpes simplex virus.

    abstract::In this study, we synthesized antisense oligodeoxynucleotides (ODNs) with phosphodiester, phosphorothioate (S-ODNs), or methylphosphonate linkages complementary to the splicing acceptor site of immediate-early pre-mRNA 5 of herpes simplex virus type 1 (HSV-1). The antiviral activity of each analog on cytopathic effect...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.40.7.1670

    authors: Shoji Y,Shimada J,Mizushima Y,Iwasawa A,Nakamura Y,Inouye K,Azuma T,Sakurai M,Nishimura T

    更新日期:1996-07-01 00:00:00

  • Effect of N-formimidoyl thienamycin (MK0787) on beta-lactamases and activity against beta-lactamase-producing strains.

    abstract::N-Formimidoyl thienamycin (MK0787) was active against beta-lactamase-producing strains and was an effective inhibitor of beta-lactamases extracted and purified from these strains except for plasmid-mediated penicillinase type IV. ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.18.5.837

    authors: Toda M,Sato K,Nakazawa H,Inoue M,Mitsuhashi S

    更新日期:1980-11-01 00:00:00

  • Predictors of mortality in patients with bloodstream infection due to ceftazidime-resistant Klebsiella pneumoniae.

    abstract::Bloodstream infection (BSI) due to multidrug-resistant Klebsiella is associated with high rates of morbidity and mortality. The aim of this study was to identify predictors of in-hospital mortality among patients with BSI due to ceftazidime-resistant (CAZ-R) Klebsiella pneumoniae at a tertiary care medical center. Pat...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.50.5.1715-1720.2006

    authors: Anderson DJ,Engemann JJ,Harrell LJ,Carmeli Y,Reller LB,Kaye KS

    更新日期:2006-05-01 00:00:00

  • Mycobacterium tuberculosis gyrase inhibitors as a new class of antitubercular drugs.

    abstract::One way to speed up the TB drug discovery process is to search for antitubercular activity among compound series that already possess some of the key properties needed in anti-infective drug discovery, such as whole-cell activity and oral absorption. Here, we present MGIs, a new series of Mycobacterium tuberculosis gy...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.03913-14

    authors: Blanco D,Perez-Herran E,Cacho M,Ballell L,Castro J,González Del Río R,Lavandera JL,Remuiñán MJ,Richards C,Rullas J,Vázquez-Muñiz MJ,Woldu E,Zapatero-González MC,Angulo-Barturen I,Mendoza A,Barros D

    更新日期:2015-04-01 00:00:00

  • In vitro activity of wALADin benzimidazoles against different life cycle stages of Plasmodium parasites.

    abstract::wALADin1 benzimidazoles are specific inhibitors of δ-aminolevulinic acid dehydratase from Wolbachia endobacteria of filarial nematodes. We report that wALADin1 and two derivatives killed blood stage Plasmodium falciparum in vitro (50% inhibitory concentrations, 39, 7.7, and 12.8 μM, respectively). One of these derivat...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02383-14

    authors: Lentz CS,Sattler JM,Fendler M,Gottwalt S,Halls VS,Strassel S,Arriens S,Hannam JS,Specht S,Famulok M,Mueller AK,Hoerauf A,Pfarr KM

    更新日期:2015-01-01 00:00:00

  • Impregnated disk method for antifungal antibiotic testing.

    abstract::Sixteen clinical fungal isolates were tested for antibiotic susceptibility by using disks impregnated with growth medium and antibiotic. The procedure was easier to perform, less time consuming, and as reliable as other currently available methods. ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.9.6.1070

    authors: Boyer JE

    更新日期:1976-06-01 00:00:00

  • A novel C5a-derived immunobiotic peptide reduces Streptococcus agalactiae colonization through targeted bacterial killing.

    abstract::Streptococcus agalactiae (group B Streptococcus [GBS]) is a Gram-positive bacterium that colonizes the cervicovaginal tract in approximately 25% of healthy women. Although colonization is asymptomatic, GBS can be vertically transmitted to newborns peripartum, causing severe disease such as pneumonia and meningitis. Cu...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01590-13

    authors: Cavaco CK,Patras KA,Zlamal JE,Thoman ML,Morgan EL,Sanderson SD,Doran KS

    更新日期:2013-11-01 00:00:00

  • Evaluation of a new line probe assay for rapid identification of gyrA mutations in Mycobacterium tuberculosis.

    abstract::Resistance of Mycobacterium tuberculosis to fluoroquinolones (FQ) results mostly from mutations in the gyrA gene. We developed a reverse hybridization-based line probe assay in which oligonucleotide probes carrying the wild-type gyrA sequence, a serine-to-threonine (S95T) polymorphism, and gyrA mutations (A90V, A90V-S...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.49.7.2928-2933.2005

    authors: Giannoni F,Iona E,Sementilli F,Brunori L,Pardini M,Migliori GB,Orefici G,Fattorini L

    更新日期:2005-07-01 00:00:00

  • Fitness cost of VanA-type vancomycin resistance in methicillin-resistant Staphylococcus aureus.

    abstract::We have quantified the biological cost of VanA-type glycopeptide resistance due to the acquisition of the resistance operon by methicillin-resistant Staphylococcus aureus (MRSA) from Enterococcus sp. Exponential growths of recipient strain HIP11713, its transconjugant VRSA-1, VRSA-5, and VRSA-6 were compared in the ab...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01702-08

    authors: Foucault ML,Courvalin P,Grillot-Courvalin C

    更新日期:2009-06-01 00:00:00

  • Molecular Epidemiology and Genome Dynamics of New Delhi Metallo-β-Lactamase-Producing Extraintestinal Pathogenic Escherichia coli Strains from India.

    abstract::The global dissemination and increasing incidence of carbapenem-resistant, Gram-negative organisms have resulted in acute public health concerns. Here, we present a retrospective multicenter study on molecular characterization of metallo-β-lactamase (MBL)-producing clinical Escherichia coli isolates recovered from ext...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01345-16

    authors: Ranjan A,Shaik S,Mondal A,Nandanwar N,Hussain A,Semmler T,Kumar N,Tiwari SK,Jadhav S,Wieler LH,Ahmed N

    更新日期:2016-10-21 00:00:00

  • Accumulation of a newly developed fluoroquinolone, OPC-17116, by human polymorphonuclear leukocytes.

    abstract::The accumulation of OPC-17116 by human polymorphonuclear leukocytes was studied by comparison with three other new quinolones, ofloxacin, levofloxacin, and DR-3354. The intracellular/extracellular concentration ratio was the highest for OPC-17116, being 66.2, followed by 9.8 for levofloxacin, 7.6 for ofloxacin, and 5....

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.37.9.1877

    authors: Taira K,Koga H,Kohno S

    更新日期:1993-09-01 00:00:00