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
  • Inhibition of Marburg Virus RNA Synthesis by a Synthetic Anti-VP35 Antibody.

    abstract：:Marburg virus causes sporadic outbreaks of severe hemorrhagic fever with high case fatality rates. Approved, effective, and safe therapeutic or prophylactic countermeasures are lacking. To address this, we used phage display to engineer a synthetic antibody, sFab H3, which binds the Marburg virus VP35 protein (mVP35)....

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00091

    authors： Amatya P,Wagner N,Chen G,Luthra P,Shi L,Borek D,Pavlenco A,Rohrs H,Basler CF,Sidhu SS,Gross ML,Leung DW

    更新日期：2019-08-09 00:00:00

  • REP 2139: Antiviral Mechanisms and Applications in Achieving Functional Control of HBV and HDV Infection.

    abstract：:Nucleic acid polymers (NAPs) are broad spectrum antiviral agents whose antiviral activity in hepatitis B virus (HBV) infection is derived from their ability to block the release of the hepatitis B virus surface antigen (HBsAg). This pharmacological activity blocks replenishment of HBsAg in the circulation, allowing ho...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章,评审

    doi：10.1021/acsinfecdis.8b00156

    authors： Vaillant A

    更新日期：2019-05-10 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

  • Combining 25-Hydroxycholesterol with an HIV Fusion Inhibitor Peptide: Interaction with Biomembrane Model Systems and Human Blood Cells.

    abstract：:The fusion between the viral and the target cell membrane is a crucial step in the life cycle of enveloped viruses. The blocking of this process is a well-known therapeutic approach that led to the development of the fusion inhibitor peptide enfuvirtide, clinically used against human immunodeficiency virus (HIV) type ...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.8b00321

    authors： Gomes B,Sanna G,Madeddu S,Hollmann A,Santos NC

    更新日期：2019-04-12 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

  • 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

  • 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

  • A Mitochondrial Orthologue of the dNTP Triphosphohydrolase SAMHD1 Is Essential and Controls Pyrimidine Homeostasis in Trypanosoma brucei.

    abstract：:The maintenance of deoxyribonucleotide triphosphate (dNTP) homeostasis through synthesis and degradation is critical for accurate genomic and mitochondrial DNA replication fidelity. Trypanosoma brucei makes use of both the salvage and de novo pathways for the provision of pyrimidine dNTPs. In this respect, the sterile...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.0c00551

    authors： Yagüe-Capilla M,Castillo-Acosta VM,Bosch-Navarrete C,Ruiz-Pérez LM,González-Pacanowska D

    更新日期：2021-01-08 00:00:00

  • Staphylococcus aureus Specific FRET Probe-Based Antibacterial Susceptibility Testing (SF-AST) by Detection of Micrococcal Nuclease Activity.

    abstract：:In this study, we describe a simple and rapid antibacterial susceptibility testing (AST) method for Staphylococcus aureus called S. aureus specific fluorescence resonance energy transfer (FRET) probe-based AST (SF-AST), which is based on an S. aureus specific FRET probe (SF probe) that detects micrococcal nuclease (MN...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00260

    authors： Yi SY,Jeong J,Kim KE,Park K,Shin YB

    更新日期：2020-02-14 00:00:00

  • Antagonizing Vancomycin Resistance in Enterococcus by Surface Localized Antimicrobial Display-Derived Peptides.

    abstract：:Decreasing the therapeutic pipeline for vancomycin-resistant Enterococci (VRE) calls for novel strategies to enhance our antibacterial arsenal. Herein, we investigated the potential applications of surface localized antimicrobial display (SLAY)-derived cationic peptides in the fight against VanA operon mediated vancom...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.9b00164

    authors： Liu Y,Jia Y,Yang K,Li R,Xiao X,Wang Z

    更新日期：2020-05-08 00:00:00

  • Investigational Studies on a Hit Compound Cyclopropane-Carboxylic Acid Derivative Targeting O-Acetylserine Sulfhydrylase as a Colistin Adjuvant.

    abstract：:Antibacterial adjuvants are of great significance, since they allow the therapeutic dose of conventional antibiotics to be lowered and reduce the insurgence of antibiotic resistance. Herein, we report that an O-acetylserine sulfhydrylase (OASS) inhibitor can be used as a colistin adjuvant to treat infections caused by...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.0c00378

    authors： Annunziato G,Spadini C,Franko N,Storici P,Demitri N,Pieroni M,Flisi S,Rosati L,Iannarelli M,Marchetti M,Magalhaes J,Bettati S,Mozzarelli A,Cabassi CS,Campanini B,Costantino G

    更新日期：2021-01-29 00:00:00

  • Global Profiling and Inhibition of Protein Lipidation in Vector and Host Stages of the Sleeping Sickness Parasite Trypanosoma brucei.

    abstract：:The enzyme N-myristoyltransferase (NMT) catalyzes the essential fatty acylation of substrate proteins with myristic acid in eukaryotes and is a validated drug target in the parasite Trypanosoma brucei, the causative agent of African trypanosomiasis (sleeping sickness). N-Myristoylation typically mediates membrane loca...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.6b00034

    authors： Wright MH,Paape D,Price HP,Smith DF,Tate EW

    更新日期：2016-06-10 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

  • 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

  • Violacein Targets the Cytoplasmic Membrane of Bacteria.

    abstract：:Violacein is a tryptophan-derived purple pigment produced by environmental bacteria, which displays multiple biological activities, including strong inhibition of Gram-positive pathogens. Here, we applied a combination of experimental approaches to identify the mechanism by which violacein kills Gram-positive bacteria...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.8b00245

    authors： Cauz ACG,Carretero GPB,Saraiva GKV,Park P,Mortara L,Cuccovia IM,Brocchi M,Gueiros-Filho FJ

    更新日期：2019-04-12 00:00:00

  • High-Throughput Luciferase-Based Assay for the Discovery of Therapeutics That Prevent Malaria.

    abstract：:In order to identify the most attractive starting points for drugs that can be used to prevent malaria, a diverse chemical space comprising tens of thousands to millions of small molecules may need to be examined. Achieving this throughput necessitates the development of efficient ultra-high-throughput screening metho...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.5b00143

    authors： Swann J,Corey V,Scherer CA,Kato N,Comer E,Maetani M,Antonova-Koch Y,Reimer C,Gagaring K,Ibanez M,Plouffe D,Zeeman AM,Kocken CH,McNamara CW,Schreiber SL,Campo B,Winzeler EA,Meister S

    更新日期：2016-04-08 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

  • Bioorganic Investigation of Multicationic Antimicrobials to Combat QAC-Resistant Staphylococcus aureus.

    abstract：:Quaternary ammonium compounds (QACs) have historically served as a first line of defense against pathogenic bacteria. Recent reports have shown that QAC resistance is increasing at an alarming rate, especially among methicillin-resistant Staphylococcus aureus (MRSA), and preliminary work has suggested that the number ...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.5b00032

    authors： Jennings MC,Buttaro BA,Minbiole KP,Wuest WM

    更新日期：2015-07-10 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

  • 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

  • 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

  • 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

  • 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

  • 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

  • Detection of Bacterial Coinfection in COVID-19 Patients Is a Missing Piece of the Puzzle in the COVID-19 Management in Indonesia.

    abstract：:Bacterial coinfection in COVID-19 patients has the potential to complicate treatments and accelerate the development of antibiotic resistance in the clinic due to the widespread use of broad-spectrum antibiotics, including in Indonesia. The surge of COVID-19 patients may worsen antibiotic overuse; therefore, informati...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.1c00006

    authors： Prasetyoputri A

    更新日期：2021-01-27 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

  • Synergistic Effect of Combined Artesunate and Tetramethylpyrazine in Experimental Cerebral Malaria.

    abstract：:Intravenous artesunate is effective against cerebral malaria (CM), but high mortality and neurological sequelae in survivors are inevitable. We investigated the effect of combined artesunate and tetramethylpyrazine using mouse models of experimental cerebral malaria (ECM). Artesunate + tetramethylpyrazine reduced micr...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.0c00124

    authors： Jiang X,Chen L,Zheng Z,Chen Y,Weng X,Guo Y,Li K,Yang T,Qu S,Liu H,Li Y,Zhu X

    更新日期：2020-09-11 00:00:00

  • Diaza-anthracene Antibiotics from a Freshwater-Derived Actinomycete with Selective Antibacterial Activity toward Mycobacterium tuberculosis.

    abstract：:Multidrug- and extensively drug-resistant strains of Mycobacterium tuberculosis are resistant to first- and second-line drug regimens and resulted in 210,000 fatalities in 2013. In the current study, we screened a library of aquatic bacterial natural product fractions for their ability to inhibit this pathogen. A frac...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章

    doi：10.1021/acsinfecdis.5b00005

    authors： Mullowney MW,Hwang CH,Newsome AG,Wei X,Tanouye U,Wan B,Carlson S,Barranis NJ,hAinmhire E,Chen WL,Krishnamoorthy K,White J,Blair R,Lee H,Burdette JE,Rathod PK,Parish T,Cho S,Franzblau SG,Murphy BT

    更新日期：2015-04-10 00:00:00

  • Using in Vitro Evolution and Whole Genome Analysis To Discover Next Generation Targets for Antimalarial Drug Discovery.

    abstract：:Although many new anti-infectives have been discovered and developed solely using phenotypic cellular screening and assay optimization, most researchers recognize that structure-guided drug design is more practical and less costly. In addition, a greater chemical space can be interrogated with structure-guided drug de...

    journal_title：ACS infectious diseases

    pub_type： 杂志文章,评审

    doi：10.1021/acsinfecdis.7b00276

    authors： Luth MR,Gupta P,Ottilie S,Winzeler EA

    更新日期：2018-03-09 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