Facilitating Compound Entry as a Means to Discover Antibiotics for Gram-Negative Bacteria

Impact of difficult-to-treat resistance in gram-negative bacteremia on mortality: retrospective analysis of nationwide surveillance data

(2020) Kyungmin Huh et al.   CLINICAL INFECTIOUS DISEASES

A Gram-Negative Antibiotic Active Through Inhibition of an Essential Riboswitch

(2020) Stephen E. Motika et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Discovery of Pyrido[2,3-b]indole Derivatives with Gram-negative Activity Targeting Both DNA Gyrase and Topoisomerase IV

(2020) Yimin Hu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Effects of antibiotic treatment on gut microbiota and how to overcome its negative impacts on human health

(2020) Camila Fontoura Acosta Ribeiro et al.   ACS Infectious Diseases

Periplasmic targets for the development of effective antimicrobials against gram-negative bacteria

(2020) Ankit Pandeya et al.   ACS Infectious Diseases

Antibacterial Discovery: 21st Century Challenges

(2020) Paul S. Hoffman   Antibiotics-Basel

Polymyxins resistance among Gram-negative pathogens in India

(2020) Hariharan Periasamy et al.   LANCET INFECTIOUS DISEASES

Defining new chemical space for drug penetration into Gram-negative bacteria

(2020) Shibin Zhao et al.   Nature Chemical Biology

Compound Uptake into E. coli Can Be Facilitated by N-Alkyl Guanidiniums and Pyridiniums

(2020) Sarah J. Perlmutter et al.   ACS Infectious Diseases

Engineering Atypical Tetracycline Formation in Amycolatopsis sulphurea for the Production of Modified Chelocardin Antibiotics

(2019) Tadeja Lukežič et al.   ACS Chemical Biology

First-generation structure-activity relationship studies of 2,3,4,9-tetrahydro-1H-carbazol-1-amines as CpxA phosphatase inhibitors

(2019) Yangxiong Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Optimization and Mechanistic Characterization of Pyridopyrimidine Inhibitors of Bacterial Biotin Carboxylase

(2019) Logan Dane Andrews et al.   JOURNAL OF MEDICINAL CHEMISTRY

Optimization of LpxC Inhibitors for Antibacterial Activity and Cardiovascular Safety

(2019) Frederick Cohen et al.   ChemMedChem

Switching on the activity of 1,5-diaryl-pyrrole derivatives against drug-resistant ESKAPE bacteria: Structure-activity relationships and mode of action studies

(2019) Domiziana Masci et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A new antibiotic selectively kills Gram-negative pathogens

(2019) Yu Imai et al.   NATURE

Implementation of permeation rules leads to a FabI inhibitor with activity against Gram-negative pathogens

(2019) Erica N. Parker et al.   Nature Microbiology

The challenge of converting Gram-positive-only compounds into broad-spectrum antibiotics

(2018) Michelle F. Richter et al.   Annals of the New York Academy of Sciences

Discovery and development of new antibacterial drugs: learning from experience?

(2018) Nicole Jackson et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Multidrug efflux pumps: structure, function and regulation

(2018) Dijun Du et al.   NATURE REVIEWS MICROBIOLOGY

Cell-based screen for discovering lipopolysaccharide biogenesis inhibitors

(2018) Ge Zhang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Riboswitches and Translation Control

(2018) Ronald R. Breaker   Cold Spring Harbor Perspectives in Biology

Antibacterial Drug Discovery: Some Assembly Required

(2018) Rubén Tommasi et al.   ACS Infectious Diseases

Quantifying the Evolutionary Conservation of Genes Encoding Multidrug Efflux Pumps in the ESKAPE Pathogens To Identify Antimicrobial Drug Targets

(2018) Lauren E. Brooks et al.   mSystems

Optimized arylomycins are a new class of Gram-negative antibiotics

(2018) Peter A. Smith et al.   NATURE

Attributable deaths and disability-adjusted life-years caused by infections with antibiotic-resistant bacteria in the EU and the European Economic Area in 2015: a population-level modelling analysis

(2018) Alessandro Cassini et al.   LANCET INFECTIOUS DISEASES

Predictive compound accumulation rules yield a broad-spectrum antibiotic

(2017) Michelle F. Richter et al.   NATURE

The drug-resistant bacteria that pose the greatest health threats

(2017) Cassandra Willyard   NATURE

Nephrotoxicity of Polymyxins: Is There Any Difference between Colistimethate and Polymyxin B?

(2016) Alexandre P. Zavascki et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Access to a Structurally Complex Compound Collection via Ring Distortion of the Alkaloid Sinomenine

(2016) Alfredo Garcia et al.   ORGANIC LETTERS

Progress against Escherichia coli with the Oxazolidinone Class of Antibacterials: Test Case for a General Approach To Improving Whole-Cell Gram-Negative Activity

(2016) Khuloud Takrouri et al.   ACS Infectious Diseases

Selective small-molecule inhibition of an RNA structural element

(2015) John A. Howe et al.   NATURE

ESKAPEing the labyrinth of antibacterial discovery

(2015) Ruben Tommasi et al.   NATURE REVIEWS DRUG DISCOVERY

Deoxynybomycins inhibit mutant DNA gyrase and rescue mice infected with fluoroquinolone-resistant bacteria

(2015) Elizabeth I. Parkinson et al.   Nature Communications

In vitro and in vivo screening for novel essential cell-envelope proteins in Pseudomonas aeruginosa

(2015) Regina Fernández-Piñar et al.   Scientific Reports

General Platform for Systematic Quantitative Evaluation of Small-Molecule Permeability in Bacteria

(2014) Tony D. Davis et al.   ACS Chemical Biology

Synthesis of Bridged Oxafenestranes from Pleuromutilin

(2014) Robert W. Hicklin et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery of azetidine based ene-amides as potent bacterial enoyl ACP reductase (FabI) inhibitors

(2014) Mohamed Takhi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Trends and Exceptions of Physical Properties on Antibacterial Activity for Gram-Positive and Gram-Negative Pathogens

(2014) Dean G. Brown et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of Complex and Diverse Compounds through Ring Distortion of Abietic Acid

(2013) Ryan J. Rafferty et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery of Inhibitors of 4′-Phosphopantetheine Adenylyltransferase (PPAT) To Validate PPAT as a Target for Antibacterial Therapy

(2013) Boudewijn L. M. de Jonge et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Novel topoisomerase inhibitors: microbiological characterisation and in vivo efficacy of pyrimidines

(2013) Maria Uria-Nickelsen et al.   INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

A ring-distortion strategy to construct stereochemically complex and structurally diverse compounds from natural products

(2013) Robert W. Huigens III et al.   Nature Chemistry

Platforms for antibiotic discovery

(2013) Kim Lewis   NATURE REVIEWS DRUG DISCOVERY

In Vivo Validation of Thymidylate Kinase (TMK) with a Rationally Designed, Selective Antibacterial Compound

(2012) Thomas A. Keating et al.   ACS Chemical Biology

Involvement of the AcrAB-TolC Efflux Pump in the Resistance, Fitness, and Virulence of Enterobacter cloacae

(2012) Astrid Pérez et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Mode of Action,In VitroActivity, andIn VivoEfficacy of AFN-1252, a Selective Antistaphylococcal FabI Inhibitor

(2012) Nachum Kaplan et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Colistin: an update on the antibiotic of the 21st century

(2012) Silpak Biswas et al.   Expert Review of Anti-Infective Therapy

Curing bacteria of antibiotic resistance: reverse antibiotics, a novel class of antibiotics in nature

(2012) Keiichi Hiramatsu et al.   INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

Challenges of Antibacterial Discovery

(2011) L. L. Silver   CLINICAL MICROBIOLOGY REVIEWS

Challenges of antibacterial discovery revisited

(2010) Michael N. Gwynn et al.   Annals of the New York Academy of Sciences

AFN-1252, a FabI Inhibitor, Demonstrates a Staphylococcus-Specific Spectrum of Activity

(2009) J. A. Karlowsky et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Triclosan Resistance of Pseudomonas aeruginosa PAO1 Is Due to FabV, a Triclosan-Resistant Enoyl-Acyl Carrier Protein Reductase

(2009) L. Zhu et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Development of a liquid chromatography/mass spectrometry-based drug accumulation assay in Pseudomonas aeruginosa

(2008) Hongliang Cai et al.   ANALYTICAL BIOCHEMISTRY

Determination of Antibiotic Hypersensitivity among 4,000 Single-Gene-Knockout Mutants of Escherichia coli

(2008) C. Tamae et al.   JOURNAL OF BACTERIOLOGY

Federal Funding for the Study of Antimicrobial Resistance in Nosocomial Pathogens: No ESKAPE

(2008) Louis B. Rice   JOURNAL OF INFECTIOUS DISEASES

Physicochemical Properties of Antibacterial Compounds: Implications for Drug Discovery

(2008) Rosemarie O’Shea et al.   JOURNAL OF MEDICINAL CHEMISTRY