当前位置： SCI文献检索 > ACS Infectious Diseases期刊下所有文献 > Novel Mercapto Propionamide Derivatives with Potent New Delhi Metallo-β-Lactamase-1 Inhibitory Activity and Low Toxicity.

Novel Mercapto Propionamide Derivatives with Potent New Delhi Metallo-β-Lactamase-1 Inhibitory Activity and Low Toxicity.

Abstract：

:The emergence and worldwide prevalence of New Delhi metallo-β-lactamase 1 (NDM-1) expressing Gram-negative bacteria with resistance against most β-lactam antibiotics pose a serious threat to human health. However, no NDM-1 inhibitors are clinically approved at present. Herein, based on the lead compound captopril, a series of compounds were designed, synthesized, and evaluated for NDM-1 inhibitory activities. All designed compounds showed single digit micromolar or submicromolar NDM-1 inhibitory activities, which were much more potent than that of captopril. Among them, compounds 14a and 14m exhibited excellent NDM-1 inhibitory activities, with IC50 values of 0.10 and 0.12 μM, respectively. Further studies demonstrated that compound 14m displayed low cytotoxicity, good water solubility, high metabolic stability, and low acute toxicity in mice. Importantly, compound 14m exhibited potent synergistic antimicrobial activities with Meropenem (MEM) for the treatment of clinically isolated NDM-1-expressing strains.

journal_name

ACS Infect Dis

journal_title

ACS infectious diseases

authors

Meng Z,Tang ML,Yu L,Liang Y,Han J,Zhang C,Hu F,Yu JM,Sun X

doi

10.1021/acsinfecdis.8b00366

subject

Has Abstract

pub_date

2019-06-14 00:00:00

pages

903-916

issue

6

issn

2373-8227

journal_volume

5

pub_type

杂志文章

相关文献

ACS Infectious Diseases文献大全
  • 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

  • Getting Drugs through Small Pores: Exploiting the Porins Pathway in Pseudomonas aeruginosa.

    abstract：:Understanding molecular properties of outer membrane channels of Gram-negative bacteria is of fundamental significance as they are the entry point of polar antibiotics into bacteria. Outer membrane proteomics revealed OccK8 (OprE) to be among the five most expressed substrate specific channels of the clinically import...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.8b00149

    authors： Samanta S,Bodrenko I,Acosta-Gutiérrez S,D'Agostino T,Pathania M,Ghai I,Schleberger C,Bumann D,Wagner R,Winterhalter M,van den Berg B,Ceccarelli M

    更新日期：2018-10-12 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

  • 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

  • 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

  • Rapid in Vitro Assessment of Clostridioides difficile Inhibition by Probiotics Using Dielectrophoresis to Quantify Cell Structure Alterations.

    abstract：:Clostridioides difficile (C. difficile) infection (CDI) is the primary cause of nosocomial antibiotic-associated diarrhea, with high recurrence rates following initial antibiotic treatment regimens. Restoration of the host gut microbiome through probiotic therapy is under investigation to reduce recurrence. Current in...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00415

    authors： Moore JH,Honrado C,Stagnaro V,Kolling G,Warren CA,Swami NS

    更新日期：2020-05-08 00:00:00

  • Discovery and Mechanistic Study of a Novel Human-Stimulator-of-Interferon-Genes Agonist.

    abstract：:Stimulator of interferon genes (STING) is an integral ER-membrane protein that can be activated by 2'3'-cGAMP synthesized by cyclic guanosine monophosphate-adenosine monophosphate synthase (cGAS) upon binding of double-stranded DNA. It activates interferon (IFN) and inflammatory cytokine responses to defend against in...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00010

    authors： Zhang X,Liu B,Tang L,Su Q,Hwang N,Sehgal M,Cheng J,Ma J,Zhang X,Tan Y,Zhou Y,Duan Z,DeFilippis VR,Viswanathan U,Kulp J,Du Y,Guo JT,Chang J

    更新日期：2019-07-12 00:00:00

  • 6-Hydroxydopamine Inhibits the Hepatitis C Virus through Alkylation of Host and Viral Proteins and the Induction of Oxidative Stress.

    abstract：:Many viruses, including the hepatitis C virus (HCV), are dependent on the host RNA silencing pathway for replication. In this study, we screened small molecule probes, previously reported to disrupt loading of the RNA-induced silencing complex (RISC), including 6-hydroxydopamine (6-OHDA), suramin (SUR), and aurintrica...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.6b00098

    authors： Lafreniere MA,Powdrill MH,Singaravelu R,Pezacki JP

    更新日期：2016-11-11 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

  • Aerobactin Synthesis Proteins as Antivirulence Targets in Hypervirulent Klebsiella pneumoniae.

    abstract：:Hypervirulent Klebsiella pneumoniae (hvKp) is an underrecognized pathotype of K. pneumoniae since the majority of cases have occurred in East Asia. However, hvKp is a public health threat due to its ability to infect healthy individuals, ongoing dissemination, and acquisition of resistance determinants. hvKp-directed ...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00117

    authors： Russo TA,Gulick AM

    更新日期：2019-07-12 00:00:00

  • New Amidated 3,6-Diphenylated Imidazopyridazines with Potent Antiplasmodium Activity Are Dual Inhibitors of Plasmodium Phosphatidylinositol-4-kinase and cGMP-Dependent Protein Kinase.

    abstract：:Recent studies on 3,6-diphenylated imidazopyridazines have demonstrated impressive in vitro activity and in vivo efficacy in mouse models of malaria infection. Herein, we report the synthesis and antiplasmodium evaluation of a new series of amidated analogues and demonstrate that these compounds potently inhibit Plasm...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.0c00481

    authors： Cheuka PM,Centani L,Arendse LB,Fienberg S,Wambua L,Renga SS,Dziwornu GA,Kumar M,Lawrence N,Taylor D,Wittlin S,Coertzen D,Reader J,van der Watt M,Birkholtz LM,Chibale K

    更新日期：2021-01-08 00:00:00

  • 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

  • Overcoming an Extremely Drug Resistant (XDR) Pathogen: Avibactam Restores Susceptibility to Ceftazidime for Burkholderia cepacia Complex Isolates from Cystic Fibrosis Patients.

    abstract：:Burkholderia multivorans is a significant health threat to persons with cystic fibrosis (CF). Infections are difficult to treat as this pathogen is inherently resistant to multiple antibiotics. Susceptibility testing of isolates obtained from CF respiratory cultures revealed that single agents selected from different ...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.7b00020

    authors： Papp-Wallace KM,Becka SA,Zeiser ET,Ohuchi N,Mojica MF,Gatta JA,Falleni M,Tosi D,Borghi E,Winkler ML,Wilson BM,LiPuma JJ,Nukaga M,Bonomo RA

    更新日期：2017-07-14 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

  • 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

  • Plasma Levels of Complement Factor I and C4b Peptides Are Associated with HIV Suppression.

    abstract：:Individuals who exhibit long-term HIV suppression and CD4 T-cell preservation without antiretroviral therapy are of great interest for HIV research. There is currently no robust method for rapid identification of these "HIV controller" subjects; however, HLA-B*57 (human leukocyte antigen (major histocompatibility comp...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.7b00042

    authors： Wu B,Ouyang Z,Lyon CJ,Zhang W,Clift T,Bone CR,Li B,Zhao Z,Kimata JT,Yu XG,Hu Y

    更新日期：2017-12-08 00:00:00

  • The Bare Essentials of Antibiotic Target Validation.

    abstract：:The convergence of competitive fitness experiments and phenotypic screening would seem to be an auspicious beginning for validation of an antibacterial target. IMPDH was already identified an essential protein in Mycobacterium tuberculosis when not one, but two, groups discovered inhibitors with promising antitubercul...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.6b00185

    authors： Hedstrom L

    更新日期：2017-01-13 00:00:00

  • Proof-of-Concept Rapid Diagnostic Test for Onchocerciasis: Exploring Peptide Biomarkers and the Use of Gold Nanoshells as Reporter Nanoparticles.

    abstract：:Three O. volvulus immunogenic peptide sequences recently discovered by peptide microarray were adapted to a lateral flow assay (LFA). The LFA employs gold nanoshells as novel high-contrast reporter nanoparticles and detects a serological response against the 3 peptides, found in OvOC9384, OvOC198, and OvOC5528, respec...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.8b00031

    authors： Gonzalez-Moa MJ,Van Dorst B,Lagatie O,Verheyen A,Stuyver L,Biamonte MA

    更新日期：2018-06-08 00:00:00

  • Cholesterol Constrains the Antigenic Configuration of the Membrane-Proximal Neutralizing HIV-1 Epitope.

    abstract：:The envelope glycoprotein (Env) enables HIV-1 cell entry through fusion of host-cell and viral membranes induced by the transmembrane subunit gp41. Antibodies targeting the C-terminal sequence of the membrane-proximal external region (C-MPER) block the fusogenic activity of gp41 and achieve neutralization of divergent...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.0c00243

    authors： Torralba J,de la Arada I,Carravilla P,Insausti S,Rujas E,Largo E,Eggeling C,Arrondo JLR,Apellániz B,Nieva JL

    更新日期：2020-08-14 00:00:00

  • Clinical and Laboratory Diagnosis of SARS-CoV-2, the Virus Causing COVID-19.

    abstract：:In December 2019, a novel beta (β) coronavirus eventually named SARS-CoV-2 emerged in Wuhan, Hubei province, China, causing an outbreak of severe and even fatal pneumonia in humans. The virus has spread very rapidly to many countries across the world, resulting in the World Health Organization (WHO) to declare a pande...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章,评审

    doi：10.1021/acsinfecdis.0c00274

    authors： da Silva SJR,Silva CTAD,Guarines KM,Mendes RPG,Pardee K,Kohl A,Pena L

    更新日期：2020-09-11 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

  • Antibodies That Engage the Hemagglutinin Receptor-Binding Site of Influenza B Viruses.

    abstract：:We describe cross-reactive human antibodies recognizing influenza B viruses spanning nearly 80 years of antigenic drift. Structures show that they engage the receptor-binding site (RBS) of the viral hemagglutinin with strong similarities to their influenza A counterparts, despite structural differences between the RBS...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.0c00726

    authors： Bajic G,Harrison SC

    更新日期：2021-01-08 00:00:00

  • Identification of Trypanosoma brucei AdoMetDC Inhibitors Using a High-Throughput Mass Spectrometry-Based Assay.

    abstract：:Human African trypanosomiasis (HAT) is a fatal infectious disease caused by the eukaryotic pathogen Trypanosoma brucei (Tb). Available treatments are difficult to administer and have significant safety issues. S-Adenosylmethionine decarboxylase (AdoMetDC) is an essential enzyme in the parasite polyamine biosynthetic p...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.7b00022

    authors： Volkov OA,Cosner CC,Brockway AJ,Kramer M,Booker M,Zhong S,Ketcherside A,Wei S,Longgood J,McCoy M,Richardson TE,Wring SA,Peel M,Klinger JD,Posner BA,De Brabander JK,Phillips MA

    更新日期：2017-07-14 00:00:00

  • 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, ...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00128

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

    更新日期：2019-10-11 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

  • Substrate Tolerance of Bacterial Glycosyltransferase MurG: Novel Fluorescence-Based Assays.

    abstract：:MurG (uridine diphosphate-N-acetylglucosamine/N-acetylmuramyl-(pentapeptide) pyrophosphoryl-undecaprenol N-acetylglucosamine transferase) is an essential bacterial glycosyltransferase that catalyzes the N-acetylglucosamine (GlcNAc) transformation of lipid I to lipid II during peptidoglycan biosynthesis. Park's nucleot...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00242

    authors： Mitachi K,Yun HG,Gillman CD,Skorupinska-Tudek K,Swiezewska E,Clemons WM Jr,Kurosu M

    更新日期：2020-06-12 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

  • An "Unlikely" Pair: The Antimicrobial Synergy of Polymyxin B in Combination with the Cystic Fibrosis Transmembrane Conductance Regulator Drugs KALYDECO and ORKAMBI.

    abstract：:Novel combination therapies are desperately needed for combating lung infections caused by bacterial "superbugs". This study aimed to investigate the synergistic antibacterial activity of polymyxin B in combination with the cystic fibrosis (CF) drugs KALYDECO (ivacaftor) and ORKAMBI (ivacaftor + lumacaftor) against Gr...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.6b00035

    authors： Schneider EK,Azad MA,Han ML,Tony Zhou Q,Wang J,Huang JX,Cooper MA,Doi Y,Baker MA,Bergen PJ,Muller MT,Li J,Velkov T

    更新日期：2016-07-08 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

  • Mechanistic Evaluation of Lipopolysaccharide-Alexidine Interaction Using Spectroscopic and in Silico Approaches.

    abstract：:The increasing problem of multidrug resistance (MDR) in bacteria calls for discovery of new molecules and diagnostic methodologies that are effective against a wide range of microbial pathogens. We have studied the role of alexidine dihydrochloride (alex) as a bioaffinity ligand against lipopolysaccharide (LPS), a pat...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.8b00087

    authors： Jagtap P,Mishra R,Khanna S,Kumari P,Mittal B,Kashyap HK,Gupta S

    更新日期：2018-11-09 00:00:00