7-(Alpha-(1-methyl-4-pyridinothio)-acetamido) cephalosporanic acid.

Abstract:

:7-[alpha-(1-Methyl-4-pyridiniothio)-acetamido] cephalosporanic acid, referred to herein as BL-S 217, is a new broad-spectrum semisynthetic cephalosporin that offers several advantages over cephalothin. A comparison of the activity in vitro of these antibiotics indicates that BL-S 217 is about eightfold more effective against Streptococcus pyogenes and Diplococcus pneumoniae. Against gram-negative bacteria, BL-S 217 possesses a broader antibacterial spectrum than cephalothin, particularly against members of the Enterobacteriaceae family; e.g., BL-S 217 inhibited over 20% more strains of both Escherichia coli and Klebsiella than cephalothin and also showed some advantage in tests against Salmonella and Enterobacter. Overall, of 208 strains of Enterobacteriaceae tested, 172 were susceptible to BL-S 217 compared to 149 for cephalothin. BL-S 217 was less bound to human serum proteins than cephalothin and gave higher peak blood levels in mice after intramuscular administration. The LD(50) of BL-S 217 in mice after subcutaneous administration was in excess of 4,000 mg/kg. When administered by the same route to mice experimentally infected with cephalothin-sensitive bacterial strains, this new cephalosporin was 20 times more effective than cephalothin in S. pyogenes and D. pneumoniae infections and 3 to 4 times more efficacious in an E. coli infection. Its therapeutic efficacy was comparable to that of cephalothin in infections produced by strains of Staphylococcus aureus, Klebsiella pneumoniae, and Proteus mirabilis.

authors

Buck RE,Leitner F,Price KE

doi

10.1128/aac.1.1.67

subject

Has Abstract

pub_date

1972-01-01 00:00:00

pages

67-72

issue

1

eissn

0066-4804

issn

1098-6596

journal_volume

1

pub_type

杂志文章
  • Molecular characterization of multidrug-resistant Mycobacterium tuberculosis isolated in Nepal.

    abstract::Despite the fact that Nepal is one of the first countries globally to introduce multidrug-resistant tuberculosis (MDR-TB) case management, the number of MDR-TB cases is continuing to rise in Nepal. Rapid molecular tests applicable in this setting to identify resistant organisms would be an effective tool in reversing ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.06418-11

    authors: Poudel A,Nakajima C,Fukushima Y,Suzuki H,Pandey BD,Maharjan B,Suzuki Y

    更新日期:2012-06-01 00:00:00

  • A Two-Year Surveillance in Five Colombian Tertiary Care Hospitals Reveals High Frequency of Non-CG258 Clones of Carbapenem-Resistant Klebsiella pneumoniae with Distinct Clinical Characteristics.

    abstract::The global spread of carbapenem-resistant Klebsiella pneumoniae (CR-Kp) has been largely associated with sequence type 258 (ST258) and its related variants (clonal group 258 [CG258]). Here we describe the molecular epidemiology of CR-Kp from five tertiary care hospitals in Medellín, the second largest city in Colombia...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,多中心研究

    doi:10.1128/AAC.01775-15

    authors: Ocampo AM,Chen L,Cienfuegos AV,Roncancio G,Chavda KD,Kreiswirth BN,Jiménez JN

    更新日期:2015-10-26 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

  • Integron-Associated DfrB4, a Previously Uncharacterized Member of the Trimethoprim-Resistant Dihydrofolate Reductase B Family, Is a Clinically Identified Emergent Source of Antibiotic Resistance.

    abstract::Whole-genome sequencing of trimethoprim-resistant Escherichia coli clinical isolates identified a member of the trimethoprim-resistant type II dihydrofolate reductase gene family (dfrB). The dfrB4 gene was located within a class I integron flanked by multiple resistance genes. This arrangement was previously reported ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02665-16

    authors: Toulouse JL,Edens TJ,Alejaldre L,Manges AR,Pelletier JN

    更新日期:2017-04-24 00:00:00

  • Resistance to linezolid in a porcine Clostridium perfringens strain carrying a mutation in the rplD gene encoding the ribosomal protein L4.

    abstract::Coresistance to human reserve antibiotics can be selected by antibiotics used in veterinary medicine. A Clostridium perfringens strain isolated from pig manure was resistant to the reserve drug linezolid and, simultaneously, resistant against florfenicol and erythromycin. We detected a new mutation in a highly conserv...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01208-09

    authors: Hölzel CS,Harms KS,Schwaiger K,Bauer J

    更新日期:2010-03-01 00:00:00

  • Randomized comparison of cefepime and ceftazidime for treatment of skin, surgical wound, and complicated urinary tract infections in hospitalized subjects.

    abstract::We undertook a prospective, randomized open comparison of the broad-spectrum cephalosporins cefepime and ceftazidime in treatment of hospitalized subjects with skin or wound infections and complicated nosocomial urinary tract infections. Cefepime treatment (dosage, 2.0 g intravenously twice daily for 4 to 28 days) was...

    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.35.11.2371

    authors: Gentry LO,Rodriguez-Gomez G

    更新日期:1991-11-01 00:00:00

  • Postantibiotic effects and postantibiotic sub-MIC effects of roxithromycin, clarithromycin, and azithromycin on respiratory tract pathogens.

    abstract::Pharmacodynamic parameters have become increasingly important for the determination of the optimal dosing schedules of antibiotics. In this study, the postantibiotic effects (PAEs), the postantibiotic sub-MIC effects (PA SMEs), and the sub-MIC effects (SMEs) of roxithromycin, clarithromycin, and azithromycin on refere...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.39.1.221

    authors: Odenholt-Tornqvist I,Löwdin E,Cars O

    更新日期:1995-01-01 00:00:00

  • In vivo emergence of multidrug-resistant mutants of Pseudomonas aeruginosa overexpressing the active efflux system MexA-MexB-OprM.

    abstract::During a 6-month period, 21 pairs of Pseudomonas aeruginosa isolates susceptible (pretherapy) and resistant (posttherapy) to antipseudomonal beta-lactam antibiotics were isolated from hospitalized patients. In vivo emergence of beta-lactam resistance was associated with the overexpression of AmpC beta-lactamase in 10 ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.43.2.287

    authors: Ziha-Zarifi I,Llanes C,Köhler T,Pechere JC,Plesiat P

    更新日期:1999-02-01 00:00:00

  • Elucidating the Role of Residue 67 in IMP-Type Metallo-β-Lactamase Evolution.

    abstract::Antibiotic resistance in bacteria is ever changing and adapting, as once-novel β-lactam antibiotics are losing their efficacy, primarily due to the production of β-lactamases. Metallo-β-lactamases (MBLs) efficiently inactivate a broad range of β-lactam antibiotics, including carbapenems, and are often coexpressed with...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01651-15

    authors: LaCuran AE,Pegg KM,Liu EM,Bethel CR,Ai N,Welsh WJ,Bonomo RA,Oelschlaeger P

    更新日期:2015-12-01 00:00:00

  • Different doses of cefetamet pivoxil (Ro 15-8075) in the treatment of acute uncomplicated gonococcal urethritis in men.

    abstract::In an open, dose-finding study, a 100% cure rate was observed in patients suffering from uncomplicated gonococcal urethritis who were treated with a single oral dose of either 1.2 g (n = 10), 0.8 g (n = 11), or 0.4 g (n = 10) of cefetamet pivoxil. The MICs of cefetamet for all gonococcal strains ranged from 0.001 to 0...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.34.4.674

    authors: Tio TT,Sindhunata IR,Wagenvoort JH,Michel MF,Stolz E

    更新日期:1990-04-01 00:00:00

  • Inhibitors of delta24(25) sterol methyltransferase block sterol synthesis and cell proliferation in Pneumocystis carinii.

    abstract::Detailed analysis of the endogenous sterol content of purified Pneumocystis carinii preparations by gas-liquid chromatography coupled to mass spectrometry suggested that this parasite can both synthesize de novo steroid skeletons (to produce delta7 sterols) and take them from the infected host (leading to delta5 stero...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.41.7.1428

    authors: Urbina JA,Visbal G,Contreras LM,McLaughlin G,Docampo R

    更新日期:1997-07-01 00:00:00

  • Inhibition of synthesis of arabinogalactan by ethambutol in Mycobacterium smegmatis.

    abstract::Ethambutol at 3.0 micrograms/ml inhibited the transfer of label from D-[14C]glucose into the D-arabinose residue of arabinogalactan in whole cells of a drug-susceptible strain of Mycobacterium smegmatis. This inhibition began almost immediately after exposure of the cells to the drug. When drug-resistant M. smegmatis ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.33.9.1493

    authors: Takayama K,Kilburn JO

    更新日期:1989-09-01 00:00:00

  • In vitro antimicrobial susceptibilities of penicillinase-producing and non-penicillinase-producing strains of Neisseria gonorrhoeae isolated in Durban, South Africa.

    abstract::The in vitro susceptibilities of 22 penicillinase-producing and 32 non-penicillinase-producing strains of Neisseria gonorrhoeae to 13 antimicrobial agents, including the new semisynthetic penicillins and cephalosporins, are reported. Ceftriaxone, ceftazidime, and cefotaxime were the most active agents tested; none of ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.26.5.770

    authors: Coovadia YM,Ramsaroop U

    更新日期:1984-11-01 00:00:00

  • Molecular Basis for the Potent Inhibition of the Emerging Carbapenemase VCC-1 by Avibactam.

    abstract::In 2016, we identified a new class A carbapenemase, VCC-1, in a nontoxigenic Vibrio cholerae strain that had been isolated from retail shrimp imported into Canada for human consumption. Shortly thereafter, seven additional VCC-1-producing V. cholerae isolates were recovered along the German coastline. These isolates a...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02112-18

    authors: Mangat CS,Vadlamani G,Holicek V,Chu M,Larmour VLC,Vocadlo DJ,Mulvey MR,Mark BL

    更新日期:2019-03-27 00:00:00

  • Targeting Human-Cytomegalovirus-Infected Cells by Redirecting T Cells Using an Anti-CD3/Anti-Glycoprotein B Bispecific Antibody.

    abstract::The host immune response to human cytomegalovirus (HCMV) is effective against HCMV reactivation from latency, though not sufficient to clear the virus. T cells are primarily responsible for the control of viral reactivation. When the host immune system is compromised, as in transplant recipients with immunosuppression...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01719-17

    authors: Meng W,Tang A,Ye X,Gui X,Li L,Fan X,Schultz RD,Freed DC,Ha S,Wang D,Zhang N,Fu TM,An Z

    更新日期:2017-12-21 00:00:00

  • Chlorhexidine resistance in methicillin-resistant Staphylococcus aureus or just an elevated MIC? An in vitro and in vivo assessment.

    abstract::Chlorhexidine (Hibiscrub; ICI) is generally accepted to be effective as an antiseptic hand wash for methicillin-susceptible Staphylococcus aureus (MSSA), but there is dispute whether the chlorhexidine MIC for methicillin-resistant S. aureus (MRSA) strains is higher than that for MSSA strains and, indeed, whether it is...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.35.10.1997

    authors: Cookson BD,Bolton MC,Platt JH

    更新日期:1991-10-01 00:00:00

  • Importation of Extensively Drug-Resistant Salmonella enterica Serovar Typhi Cases in Ontario, Canada.

    abstract::A strain of extensively drug-resistant (XDR) Salmonella enterica serovar Typhi has caused a large ongoing outbreak in Pakistan since 2016. In Ontario, Canada, 10 cases of mainly bloodstream infections (n = 9) were identified in patients who traveled to Pakistan. Whole-genome sequencing showed that Canadian cases were ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02581-19

    authors: Eshaghi A,Zittermann S,Bharat A,Mulvey MR,Allen VG,Patel SN

    更新日期:2020-04-21 00:00:00

  • Mycobacterium abscessus Smooth and Rough Morphotypes Form Antimicrobial-Tolerant Biofilm Phenotypes but Are Killed by Acetic Acid.

    abstract::Mycobacterium abscessus has emerged as an important pathogen in people with chronic inflammatory lung diseases such as cystic fibrosis, and recent reports suggest that it may be transmissible by fomites. M. abscessus exhibits two major colony morphology variants: a smooth morphotype (MaSm ) and a rough morphotype (MaR...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01782-17

    authors: Clary G,Sasindran SJ,Nesbitt N,Mason L,Cole S,Azad A,McCoy K,Schlesinger LS,Hall-Stoodley L

    更新日期:2018-02-23 00:00:00

  • Comparison of clindamycin, erythromycin, and methicillin in streptococcal infections in monkeys.

    abstract::Intravenous inoculation of a group A hemolytic streptococcus caused lethal infections in all of eight untreated monkeys. Intramuscular injections of clindamycin-2-phosphate in a daily dose of 25 mg/kg given in equal morning and afternoon doses for 10 days resulted in survival of all of eight monkeys. Similar results w...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.1.6.460

    authors: Carlisle HN,Saslaw S

    更新日期:1972-06-01 00:00:00

  • Penicillin-binding proteins of penicillin-susceptible and -resistant pneumococci: immunological relatedness of altered proteins and changes in peptides carrying the beta-lactam binding site.

    abstract::There are several major differences between the penicillin-binding proteins (PBPs) of highly penicillin-resistant and -susceptible strains of pneumococci. The highest-molecular-size PBP 1a (98 kilodaltons [kDa]) of susceptible pneumococci is not detectable in resistant bacteria. Instead, resistant strains contain a PB...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.30.4.553

    authors: Hakenbeck R,Ellerbrok H,Briese T,Handwerger S,Tomasz A

    更新日期:1986-10-01 00:00:00

  • Inhibitory effects of polyethers on human immunodeficiency virus replication.

    abstract::We examined the inhibitory activities of 10 polyether antibiotics on human immunodeficiency virus (HIV) type 1. These compounds caused concentration-dependent inhibition of HIV replication in primary infected cultures of human T-lymphoblastoid H9 cells. The ratio of 50% effective concentrations for cellular cytotoxici...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.36.2.492

    authors: Nakamura M,Kunimoto S,Takahashi Y,Naganawa H,Sakaue M,Inoue S,Ohno T,Takeuchi T

    更新日期:1992-02-01 00:00:00

  • Deoxysugars as antituberculars and alpha-mannosidase inhibitors.

    abstract::A promising modified sugar molecule was identified which was active against multidrug-resistant (MDR) strains of Mycobacterium tuberculosis, suggesting involvement of a new target. The compound was demonstrated to be bactericidal, inhibited the growth of M. tuberculosis in mice, and targeted alpha-mannosidase as a com...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02715-13

    authors: Kashyap V,Sharma S,Singh V,Sharma SK,Saquib M,Srivastava R,Shaw AK

    更新日期:2014-06-01 00:00:00

  • Mutations Reducing In Vitro Susceptibility to Novel LpxC Inhibitors in Pseudomonas aeruginosa and Interplay of Efflux and Nonefflux Mechanisms.

    abstract::Upregulated expression of efflux pumps, lpxC target mutations, LpxC protein overexpression, and mutations in fabG were previously shown to mediate single-step resistance to the LpxC inhibitor CHIR-090 in P. aeruginosa Single-step selection experiments using three recently described LpxC inhibitors (compounds 2, 3, and...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01490-19

    authors: Jones AK,Caughlan RE,Woods AL,Uehara K,Xie L,Barnes SW,Walker JR,Thompson KV,Ranjitkar S,Lee PS,Dean CR

    更新日期:2019-12-20 00:00:00

  • Biofilm compared to conventional antimicrobial susceptibility of Stenotrophomonas maltophilia Isolates from cystic fibrosis patients.

    abstract::Stenotrophomonas maltophilia is a multidrug-resistant organism increasingly isolated from the lungs of cystic fibrosis (CF) patients. One hundred twenty-five S. maltophilia isolates from 85 CF patients underwent planktonic and biofilm susceptibility testing against 9 different antibiotics, alone and in double antibiot...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02215-12

    authors: Wu K,Yau YC,Matukas L,Waters V

    更新日期:2013-03-01 00:00:00

  • Cyclic AMP signaling pathway modulates susceptibility of candida species and Saccharomyces cerevisiae to antifungal azoles and other sterol biosynthesis inhibitors.

    abstract::Azoles are widely used antifungals; however, their efficacy is compromised by fungistatic activity and selection of resistant strains during treatment. Recent studies demonstrated roles for the protein kinase C and calcium signaling pathways in modulating azole activity. Here we explored a role for the signaling pathw...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.10.3195-3201.2003

    authors: Jain P,Akula I,Edlind T

    更新日期:2003-10-01 00:00:00

  • Whole-genome sequencing of gentamicin-resistant Campylobacter coli isolated from U.S. retail meats reveals novel plasmid-mediated aminoglycoside resistance genes.

    abstract::Aminoglycoside resistance in Campylobacter has been routinely monitored in the United States in clinical isolates since 1996 and in retail meats since 2002. Gentamicin resistance first appeared in a single human isolate of Campylobacter coli in 2000 and in a single chicken meat isolate in 2007, after which it increase...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00669-13

    authors: Chen Y,Mukherjee S,Hoffmann M,Kotewicz ML,Young S,Abbott J,Luo Y,Davidson MK,Allard M,McDermott P,Zhao S

    更新日期:2013-11-01 00:00:00

  • Induction of the Citrobacter freundii group I beta-lactamase in Escherichia coli is not dependent on entry of beta-lactam into the cytoplasm.

    abstract::Induction of the cloned ampC Citrobacter freundii beta-lactamase in Escherichia coli by 6-aminopenicillanic acid was prevented by periplasmic TEM beta-lactamase in the same cell. In contrast, cytoplasmic TEM beta-lactamase did not prevent induction. This result implies that entry of the beta-lactam into the cytoplasm ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.34.12.2429

    authors: Everett MJ,Chopra I,Bennett PM

    更新日期:1990-12-01 00:00:00

  • Enhancement of the in vitro activity of amphotericin B against Aspergillus spp. by tetracycline analogs.

    abstract::Strains of Aspergillus fumigatus, Aspergillus flavus, and Aspergillus niger were tested for in vitro susceptibility to amphotericin B alone and in combination with fixed concentrations of tetracycline, doxycycline, or minocycline, using buffered minimal essential medium in microtiter plates. Enhanced inhibitory activi...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.26.6.837

    authors: Hughes CE,Harris C,Peterson LR,Gerding DN

    更新日期:1984-12-01 00:00:00

  • Detection of E119V and E119I mutations in influenza A (H3N2) viruses isolated from an immunocompromised patient: challenges in diagnosis of oseltamivir resistance.

    abstract::The clinical use of the neuraminidase inhibitor (NAI) oseltamivir is associated with the emergence of drug resistance resulting from subtype-specific neuraminidase (NA) mutations. The influenza A/Texas/12/2007 (H3N2) virus isolated from an oseltamivir-treated immunocompromised patient exhibited reduced susceptibility ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01608-09

    authors: Okomo-Adhiambo M,Demmler-Harrison GJ,Deyde VM,Sheu TG,Xu X,Klimov AI,Gubareva LV

    更新日期:2010-05-01 00:00:00

  • Activity of Cefiderocol Alone and in Combination with Levofloxacin, Minocycline, Polymyxin B, or Trimethoprim-Sulfamethoxazole against Multidrug-Resistant Stenotrophomonas maltophilia.

    abstract::The production of an L1 metallo-β-lactamase and an L2 serine active-site β-lactamase precludes the use of β-lactams for the treatment of Stenotrophomonas maltophilia infections. Preclinical data suggest that cefiderocol is the first approved β-lactam with reliable activity against S. maltophilia, but data on strains r...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00559-20

    authors: Biagi M,Vialichka A,Jurkovic M,Wu T,Shajee A,Lee M,Patel S,Mendes RE,Wenzler E

    更新日期:2020-08-20 00:00:00