当前位置： SCI文献检索 > ACS Infectious Diseases期刊下所有文献 > Modification at the 2'-Position of the 4,5-Series of 2-Deoxystreptamine Aminoglycoside Antibiotics To Resist Aminoglycoside Modifying Enzymes and Increase Ribosomal Target Selectivity.

Modification at the 2'-Position of the 4,5-Series of 2-Deoxystreptamine Aminoglycoside Antibiotics To Resist Aminoglycoside Modifying Enzymes and Increase Ribosomal Target Selectivity.

Abstract：

:A series of derivatives of the 4,5-disubstituted class of 2-deoxystreptamine aminoglycoside antibiotics neomycin, paromomycin, and ribostamycin was prepared and assayed for (i) their ability to inhibit protein synthesis by bacterial ribosomes and by engineered bacterial ribosomes carrying eukaryotic decoding A sites, (ii) antibacterial activity against wild type Gram negative and positive pathogens, and (iii) overcoming resistance due to the presence of aminoacyl transferases acting at the 2'-position. The presence of five suitably positioned residual basic amino groups was found to be necessary for activity to be retained upon removal or alkylation of the 2'-position amine. As alkylation of the 2'-amino group overcomes the action of resistance determinants acting at that position and in addition results in increased selectivity for the prokaryotic over eukaryotic ribosomes, it constitutes an attractive modification for introduction into next generation aminoglycosides. In the neomycin series, the installation of small (formamide) or basic (glycinamide) amido groups on the 2'-amino group is tolerated.

journal_name

ACS Infect Dis

journal_title

ACS infectious diseases

authors

Sati GC,Sarpe VA,Furukawa T,Mondal S,Mantovani M,Hobbie SN,Vasella A,Böttger EC,Crich D

doi

10.1021/acsinfecdis.9b00128

subject

Has Abstract

pub_date

2019-10-11 00:00:00

pages

1718-1730

issue

10

issn

2373-8227

journal_volume

5

pub_type

杂志文章

相关文献

ACS Infectious Diseases文献大全
  • Efficient Blocking of Enterovirus 71 Infection by Heparan Sulfate Analogues Acting as Decoy Receptors.

    abstract：:Enterovirus 71 (EV71) is a major etiological agent of hand, foot, and mouth disease, for which there is no antiviral therapy. We have developed densely sulfated disaccharide heparan sulfate (HS) analogues that are potent small molecule inhibitors of EV71 infection, binding to the viral capsid and acting as decoy recep...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00070

    authors： Earley DF,Bailly B,Maggioni A,Kundur AR,Thomson RJ,Chang CW,von Itzstein M

    更新日期：2019-10-11 00:00:00

  • Photodynamic Inactivation of ESKAPE Group Bacterial Pathogens in Planktonic and Biofilm Cultures Using Metallated Porphyrin-Doped Conjugated Polymer Nanoparticles.

    abstract：:Photodynamic inactivation (PDI) protocols using photoactive metallated porphyrin-doped conjugated polymer nanoparticles (CPNs) and blue light were developed to eliminate multidrug-resistant pathogens. CPNs-PDI protocols using varying particle concentrations and irradiation doses were tested against nine pathogenic bac...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.0c00268

    authors： Martínez SR,Ibarra LE,Ponzio RA,Forcone MV,Wendel AB,Chesta CA,Spesia MB,Palacios RE

    更新日期：2020-08-14 00:00:00

  • JMX0207, a Niclosamide Derivative with Improved Pharmacokinetics, Suppresses Zika Virus Infection Both In Vitro and In Vivo.

    abstract：:Flaviviruses causes significant human disease. Recent outbreaks of the Zika virus highlight the need to develop effective therapies for this class of viruses. Previously we identified niclosamide as a broad-spectrum inhibitor for flaviviruses by targeting the interface between viral protease NS3 and its cofactor NS2B....

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.0c00217

    authors： Li Z,Xu J,Lang Y,Fan X,Kuo L,D'Brant L,Hu S,Samrat SK,Trudeau N,Tharappel AM,Rugenstein N,Koetzner CA,Zhang J,Chen H,Kramer LD,Butler D,Zhang QY,Zhou J,Li H

    更新日期：2020-10-09 00:00:00

  • Toward Broad Spectrum Dihydrofolate Reductase Inhibitors Targeting Trimethoprim Resistant Enzymes Identified in Clinical Isolates of Methicillin Resistant Staphylococcus aureus.

    abstract：:The spread of plasmid borne resistance enzymes in clinical Staphylococcus aureus isolates is rendering trimethoprim and iclaprim, both inhibitors of dihydrofolate reductase (DHFR), ineffective. Continued exploitation of these targets will require compounds that can broadly inhibit these resistance-conferring isoforms....

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00222

    authors： Reeve SM,Si D,Krucinska J,Yan Y,Viswanathan K,Wang S,Holt GT,Frenkel MS,Ojewole AA,Estrada A,Agabiti SS,Alverson JB,Gibson ND,Priestley ND,Wiemer AJ,Donald BR,Wright DL

    更新日期：2019-11-08 00:00:00

  • Targeting Bacterial Sortase A with Covalent Inhibitors: 27 New Starting Points for Structure-Based Hit-to-Lead Optimization.

    abstract：:Because of its essential role as a bacterial virulence factor, enzyme sortase A (SrtA) has become an attractive target for the development of new antivirulence drugs against Gram-positive infections. Here we describe 27 compounds identified as covalent inhibitors of Staphylococcus aureus SrtA by screening a library of...

    journal_title：ACS infectious diseases

    pub_type： 信件

    doi：10.1021/acsinfecdis.9b00265

    authors： Jaudzems K,Kurbatska V,Je Kabsons A,Bobrovs R,Rudevica Z,Leonchiks A

    更新日期：2020-02-14 00:00:00

  • Enterovirus D68 Antivirals: Past, Present, and Future.

    abstract：:Enterovirus D68 (EV-D68) is an RNA virus that causes respiratory illnesses mainly in children. In severe cases, it can lead to neurological complications such as acute flaccid myelitis (AFM). EV-D68 belongs to the enterovirus genera of the Picornaviridae family, which also includes many other significant human pathoge...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.0c00120

    authors： Hu Y,Musharrafieh R,Zheng M,Wang J

    更新日期：2020-07-10 00:00:00

  • Efforts Aimed To Reduce Attrition in Antimalarial Drug Discovery: A Systematic Evaluation of the Current Antimalarial Targets Portfolio.

    abstract：:Malaria remains a major global health problem. In 2015 alone, more than 200 million cases of malaria were reported, and more than 400,000 deaths occurred. Since 2010, emerging resistance to current front-line ACTs (artemisinin combination therapies) has been detected in endemic countries. Therefore, there is an urgenc...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.7b00211

    authors： Chaparro MJ,Calderón F,Castañeda P,Fernández-Alvaro E,Gabarró R,Gamo FJ,Gómez-Lorenzo MG,Martín J,Fernández E

    更新日期：2018-04-13 00:00:00

  • Targeted Inhibition of Plasmodium falciparum Calcium-Dependent Protein Kinase 1 with a Constrained J Domain-Derived Disruptor Peptide.

    abstract：:To explore the possibility of constrained peptides to target Plasmodium-infected cells, we designed a J domain mimetic derived from Plasmodium falciparum calcium-dependent protein kinase 1 ( PfCDPK1) as a strategy to disrupt J domain binding and inhibit PfCDPK1 activity. The J domain disruptor (JDD) peptide was confor...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.8b00347

    authors： Flaherty BR,Ho TG,Schmidt SH,Herberg FW,Peterson DS,Kennedy EJ

    更新日期：2019-04-12 00:00:00

  • Biogenic and Biomimetic Carriers as Versatile Transporters To Treat Infections.

    abstract：:Biogenic and biomimetic therapeutics are a relatively new class of systems that are of physiological origin and/or take advantage of natural pathways or aim at mimicking these to improve selective interaction with target tissue. The number of biogenic and bioengineered avenues for drug therapy and diagnostics has mult...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章,评审

    doi：10.1021/acsinfecdis.8b00030

    authors： Goes A,Fuhrmann G

    更新日期：2018-06-08 00:00:00

  • Toward Curative Immunomodulation Strategies for Chronic Hepatitis B Virus Infection.

    abstract：:Chronic hepatitis B virus (HBV) infection remains a major cause of morbidity and mortality worldwide. HBV surface antigen loss is considered a functional cure and is an ideal goal for antiviral therapy. However, current treatment regimens, including nucleos(t)ide analogues or interferons monotherapy and combination th...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章,评审

    doi：10.1021/acsinfecdis.8b00297

    authors： Zhu W,Liu H,Zhang X

    更新日期：2019-05-10 00:00:00

  • Developments in Glycopeptide Antibiotics.

    abstract：:Glycopeptide antibiotics (GPAs) are a key weapon in the fight against drug resistant bacteria, with vancomycin still a mainstream therapy against serious Gram-positive infections more than 50 years after it was first introduced. New, more potent semisynthetic derivatives that have entered the clinic, such as dalbavanc...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.7b00258

    authors： Blaskovich MAT,Hansford KA,Butler MS,Jia Z,Mark AE,Cooper MA

    更新日期：2018-05-11 00:00:00

  • Zika Virus: Diagnosis, Therapeutics, and Vaccine.

    abstract：:The current explosive epidemic of Zika virus in South and Central America, as well as the Caribbean, poses a global public health emergency. Here we comment on the challenges on development of better diagnosis and potential therapeutics and vaccine for Zika virus. ...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.6b00030

    authors： Shan C,Xie X,Barrett AD,Garcia-Blanco MA,Tesh RB,Vasconcelos PF,Vasilakis N,Weaver SC,Shi PY

    更新日期：2016-03-11 00:00:00

  • Immunoassay for HIV Drug Metabolites Tenofovir and Tenofovir Diphosphate.

    abstract：:Poor patient adherence to antiretroviral medication represents a major obstacle for managing disease and reducing rates of new HIV infections. The measurement of patient drug levels is the most objective method of determining adherence. Tenofovir and tenofovir diphosphate are metabolites of some of the most common HIV...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.0c00010

    authors： Sevenler D,Bardon A,Fernandez Suarez M,Marshall L,Toner M,Drain PK,Sandlin RD

    更新日期：2020-07-10 00:00:00

  • Broad Spectrum Antiviral Agent Niclosamide and Its Therapeutic Potential.

    abstract：:The recent outbreak of coronavirus disease 2019 (COVID-19) highlights an urgent need for therapeutics. Through a series of drug repurposing screening campaigns, niclosamide, an FDA-approved anthelminthic drug, was found to be effective against various viral infections with nanomolar to micromolar potency such as SARS-...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章,评审

    doi：10.1021/acsinfecdis.0c00052

    authors： Xu J,Shi PY,Li H,Zhou J

    更新日期：2020-05-08 00:00:00

  • Repositioning of Guanabenz in Conjugation with Gold and Silver Nanoparticles against Pathogenic Amoebae Acanthamoeba castellanii and Naegleria fowleri.

    abstract：:Brain-eating amoebae cause devastating infections in the central nervous system of humans, resulting in a mortality rate of 95%. There are limited effective therapeutic options available clinically for treating granulomatous amoebic encephalitis and primary amoebic meningoencephalitis caused by Acanthamoeba castellani...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00263

    authors： Anwar A,Mungroo MR,Anwar A,Sullivan WJ Jr,Khan NA,Siddiqui R

    更新日期：2019-12-13 00:00:00

  • The Outer Membrane Protein FstC of Aeromonas salmonicida subsp. salmonicida Acts as Receptor for Amonabactin Siderophores and Displays a Wide Ligand Plasticity. Structure-Activity Relationships of Synthetic Amonabactin Analogues.

    abstract：:Amonabactins are a group of four related catecholate siderophores produced by several species of the genus Aeromonas, including A. hydrophila and the fish pathogen A. salmonicida subsp. salmonicida. Although the gene cluster encoding amonabactin biosynthesis also contains a gene that could encode the ferri-siderophore...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00274

    authors： Rey-Varela D,Cisneros-Sureda J,Balado M,Rodríguez J,Lemos ML,Jiménez C

    更新日期：2019-11-08 00:00:00

  • LRRK2 in Infection: Friend or Foe?

    abstract：:In the field of Parkinson's disease (PD) research, leucine-rich repeat kinase 2 (LRRK2) remains one of the most enigmatic kinases. LRRK2 pathogenic mutations result in increased kinase activity, making LRRK2 an attractive therapeutic target for PD. For over 10 years, the identification of a bona fide substrate and a p...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00051

    authors： Herbst S,Gutierrez MG

    更新日期：2019-06-14 00:00:00

  • Inhibiting Iron Mobilization from Bacterioferritin in Pseudomonas aeruginosa Impairs Biofilm Formation Irrespective of Environmental Iron Availability.

    abstract：:Although iron is essential for bacteria, the nutrient presents problems of toxicity and solubility. Bacteria circumvent these problems with the aid of iron storage proteins where Fe3+ is deposited and, when necessary, mobilized as Fe2+ for metabolic requirements. In Pseudomonas aeruginosa, Fe3+ is compartmentalized in...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00398

    authors： Soldano A,Yao H,Chandler JR,Rivera M

    更新日期：2020-03-13 00:00:00

  • Illicit Transport via Dipeptide Transporter Dpp is Irrelevant to the Efficacy of Negamycin in Mouse Thigh Models of Escherichia coli Infection.

    abstract：:Negamycin is a hydrophilic antimicrobial translation inhibitor that crosses the lipophilic inner membrane of Escherichia coli via at least two transport routes to reach its intracellular target. In a minimal salts medium, negamycin's peptidic nature allows illicit entry via a high-affinity route by hijacking the Dpp d...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.5b00027

    authors： McKinney DC,Bezdenejnih-Snyder N,Farrington K,Guo J,McLaughlin RE,Ruvinsky AM,Singh R,Basarab GS,Narayan S,Buurman ET

    更新日期：2015-05-08 00:00:00

  • Protein S-Palmitoylation Is Responsive to External Signals and Plays a Regulatory Role in Microneme Secretion in Plasmodium falciparum Merozoites.

    abstract：:Protein S-palmitoylation is an important post-translational modification (PTM) in blood stages of the malaria parasite, Plasmodium falciparum. S-palmitoylation refers to reversible covalent modification of cysteine residues of proteins by saturated fatty acids. In vivo, palmitoylation is regulated by concerted activit...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00321

    authors： Siddiqui MA,Singh S,Malhotra P,Chitnis CE

    更新日期：2020-03-13 00:00:00

  • Nerve Growth Factor Confers Neuroprotection against Colistin-Induced Peripheral Neurotoxicity.

    abstract：:Neurotoxicity is an unwanted side effect for patients when receiving parenteral colistin therapy. The development of effective neuroprotective agents that can be coadministered during colistin therapy remains a priority area in antimicrobial chemotherapy. The present study aimed to investigate the protective effect of...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.0c00107

    authors： Dai C,Xiong J,Wang Y,Shen J,Velkov T,Xiao X

    更新日期：2020-06-12 00:00:00

  • Effect of Composition on Antibacterial Activity of Sequence-Defined Cationic Oligothioetheramides.

    abstract：:In response to the urgent need for new antibiotic development strategies, antimicrobial peptides and their synthetic mimetics are being investigated as promising alternatives to traditional antibiotics. To facilitate their development into clinically viable candidates, we need to understand what molecular features and...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.8b00079

    authors： Artim CM,Phan NN,Alabi CA

    更新日期：2018-08-10 00:00:00

  • Probing the Interaction of Aspergillomarasmine A with Metallo-β-lactamases NDM-1, VIM-2, and IMP-7.

    abstract：:Metallo-β-lactamases (MBLs) are a growing threat to the continued efficacy of β-lactam antibiotics. Recently, aspergillomarasmine A (AMA) was identified as an MBL inhibitor, but the mode of inhibition was not fully characterized. Equilibrium dialysis and metal analysis studies revealed that 2 equiv of AMA effectively ...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.7b00106

    authors： Bergstrom A,Katko A,Adkins Z,Hill J,Cheng Z,Burnett M,Yang H,Aitha M,Mehaffey MR,Brodbelt JS,Tehrani KHME,Martin NI,Bonomo RA,Page RC,Tierney DL,Fast W,Wright GD,Crowder MW

    更新日期：2018-02-09 00:00:00

  • Phylogenetic and Biochemical Analyses of Mycobacterial l,d-Transpeptidases Reveal a Distinct Enzyme Class That Is Preferentially Acylated by Meropenem.

    abstract：:The genomes of diverse mycobacterial species encode multiple proteins with the canonical l,d-transpeptidase (Ldt) sequence motif. The reason for this apparent redundancy is not well understood, but evidence suggests paralogous Ldts may serve niche roles in maintaining and/or remodeling mycobacterial peptidoglycan. We ...

    journal_title：ACS infectious diseases

    pub_type： 信件

    doi：10.1021/acsinfecdis.9b00234

    authors： Zandi TA,Marshburn RL,Stateler PK,Brammer Basta LA

    更新日期：2019-12-13 00:00:00

  • Daptomycin Leakage Is Selective.

    abstract：:Daptomycin is a lipopeptide antibiotic approved for use against Gram-positive organisms, including highly resistant species. A number of studies have suggested that daptomycin kills bacteria by membrane permeabilization and depolarization. Recently a model membrane system consisting of 1,2-dimyristoyl-sn-glycero-3-pho...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.6b00152

    authors： Zhang J,Scoten K,Straus SK

    更新日期：2016-10-14 00:00:00

  • Investigations into the Antibacterial Mechanism of Action of Viridicatumtoxins.

    abstract：:Viridicatumtoxins are a rare class of tetracycline-like antibiotics that strongly inhibit drug-resistant Gram-positive bacteria. Although reported to exhibit in vitro inhibition activity to undecaprenyl pyrophosphate synthase (UPPS), an essential enzyme in bacterial cell wall synthesis, the biological targets and mech...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.0c00031

    authors： Li W,Li L,Zhang C,Cai Y,Gao Q,Wang F,Cao Y,Lin J,Li J,Shang Z,Lin W

    更新日期：2020-07-10 00:00:00

  • Development of Antibiotics That Dysregulate the Neisserial ClpP Protease.

    abstract：:Evolving antimicrobial resistance has motivated the search for novel targets and alternative therapies. Caseinolytic protease (ClpP) has emerged as an enticing new target since its function is conserved and essential for bacterial fitness, and because its inhibition or dysregulation leads to bacterial cell death. ClpP...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.0c00599

    authors： Binepal G,Mabanglo MF,Goodreid JD,Leung E,Barghash MM,Wong KS,Lin F,Cossette M,Bansagi J,Song B,Balasco Serrão VH,Pai EF,Batey RA,Gray-Owen SD,Houry WA

    更新日期：2020-12-11 00:00:00

  • Daptomycin Pore Formation Is Restricted by Lipid Acyl Chain Composition.

    abstract：:Daptomycin is a calcium-dependent lipopeptide antibiotic that is used clinically against various Gram-positive pathogens. It acts on bacterial cell membranes, whose susceptibility varies with the content of phosphatidylglycerol (PG). Some studies have reported that daptomycin permeabilizes and depolarizes bacterial ce...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.7b00138

    authors： Taylor R,Beriashvili D,Taylor S,Palmer M

    更新日期：2017-11-10 00:00:00

  • Antituberculosis Activity of the Antimalaria Cytochrome bcc Oxidase Inhibitor SCR0911.

    abstract：:The ability to respire and generate adenosine triphosphate (ATP) is essential for the physiology, persistence, and pathogenicity of Mycobacterium tuberculosis, which causes tuberculosis. By employing a lead repurposing strategy, the malarial cytochrome bc1 inhibitor SCR0911 was tested against mycobacteria. Docking stu...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00408

    authors： Chong SMS,Manimekalai MSS,Sarathy JP,Williams ZC,Harold LK,Cook GM,Dick T,Pethe K,Bates RW,Grüber G

    更新日期：2020-04-10 00:00:00

  • Host-Mediated Bioactivation of Pyrazinamide: Implications for Efficacy, Resistance, and Therapeutic Alternatives.

    abstract：:Pyrazinamide has played a critical role in shortening therapy against drug-sensitive, drug-resistant, active, and latent tuberculosis (TB). Despite widespread recognition of its therapeutic importance, the sterilizing properties of this 60-year-old drug remain an enigma given its rather poor activity in vitro. Here we...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/id500028m

    authors： Via LE,Savic R,Weiner DM,Zimmerman MD,Prideaux B,Irwin SM,Lyon E,O'Brien P,Gopal P,Eum S,Lee M,Lanoix JP,Dutta NK,Shim T,Cho JS,Kim W,Karakousis PC,Lenaerts A,Nuermberger E,Barry CE 3rd,Dartois V

    更新日期：2015-05-08 00:00:00