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ESKAPEing the labyrinth of antibacterial discovery

Nature reviews. Drug discovery, 2015-08, Vol.14 (8), p.529-542

2015

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

Journal of medicinal chemistry, 2014-12, Vol.57 (23), p.10144-10161

2014

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In vivo dose response and efficacy of the β-lactamase inhibitor, durlobactam, in combination with sulbactam against the Acinetobacter baumannii-calcoaceticus complex

Antimicrobial agents and chemotherapy, 2024-01, Vol.68 (1), p.e0080023-e0080023

2024

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Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors

Bioorganic & medicinal chemistry, 2011-08, Vol.19 (15), p.4626-4634

2011

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N-Hydroxyformamide LpxC inhibitors, their in vivo efficacy in a mouse Escherichia coli infection model, and their safety in a rat hemodynamic assay

Bioorganic & medicinal chemistry, 2020-12, Vol.28 (24), p.115826-115826, Article 115826

2020

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Rational design of a new antibiotic class for drug-resistant infections

Nature (London), 2021-09, Vol.597 (7878), p.698-702

2021

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Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β‑Lactamases

Journal of medicinal chemistry, 2020-11, Vol.63 (21), p.12511-12525

2020

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Identification of broad-spectrum antiviral compounds and assessment of the druggability of their target for efficacy against respiratory syncytial virus (RSV)

Proceedings of the National Academy of Sciences - PNAS, 2011-04, Vol.108 (17), p.6739-6744

2011

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Antibacterial Drug Discovery: Some Assembly Required

ACS infectious diseases, 2018-05, Vol.4 (5), p.686-695

2018

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Optimization of Halopemide for Phospholipase D2 inhibition

Bioorganic & medicinal chemistry letters, 2007-04, Vol.17 (8), p.2310-2311

2007

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Tipranavir (PNU-140690): A Potent, Orally Bioavailable Nonpeptidic HIV Protease Inhibitor of the 5,6-Dihydro-4-hydroxy-2-pyrone Sulfonamide Class

Journal of medicinal chemistry, 1998-08, Vol.41 (18), p.3467-3476

1998

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Discovery of Potent, Selective, and Orally Active Carboxylic Acid Based Inhibitors of Matrix Metalloproteinase-13

Journal of medicinal chemistry, 2009-06, Vol.52 (11), p.3523-3538

2009

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Identification of Dipeptidyl Nitriles as Potent and Selective Inhibitors of Cathepsin B through Structure-Based Drug Design

Journal of medicinal chemistry, 2001-12, Vol.44 (26), p.4524-4534

2001

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Potent and selective 2-naphthylsulfonamide substituted hydroxamic acid inhibitors of matrix metalloproteinase-13

Bioorganic & medicinal chemistry letters, 2011-11, Vol.21 (21), p.6440-6445

2011

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Biophysical Investigation of the Mode of Inhibition of Tetramic Acids, the Allosteric Inhibitors of Undecaprenyl Pyrophosphate Synthase

Biochemistry (Easton), 2010-06, Vol.49 (25), p.5366-5376

2010

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Challenges and opportunities in the discovery, development, and commercialization of pathogen-targeted antibiotics

Drug discovery today, 2021-09, Vol.26 (9), p.2084-2089

2021

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Role of the Klebsiella pneumoniae TolC porin in antibiotic efflux

Research in microbiology, 2019-03, Vol.170 (2), p.112-116

2019

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Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases

Scientific reports, 2015-07, Vol.5 (1), p.11827, Article 11827

2015

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Pharmacokinetic/Pharmacodynamic Determination and Preclinical Pharmacokinetics of the β-Lactamase Inhibitor ETX1317 and Its Orally Available Prodrug ETX0282

ACS infectious diseases, 2020-06, Vol.6 (6), p.1378-1388

2020

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Acinetobacter baumannii OmpA Is a Selective Antibiotic Permeant Porin

ACS infectious diseases, 2018-03, Vol.4 (3), p.373-381

2018

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Design, Synthesis, and Properties of a Potent Inhibitor of Pseudomonas aeruginosa Deacetylase LpxC

Journal of medicinal chemistry, 2017-06, Vol.60 (12), p.5002-5014

2017

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N-Arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B

Bioorganic & medicinal chemistry letters, 2003-11, Vol.13 (22), p.4121-4124

2003

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4‑Aminoquinolone Piperidine Amides: Noncovalent Inhibitors of DprE1 with Long Residence Time and Potent Antimycobacterial Activity

Journal of medicinal chemistry, 2014-06, Vol.57 (12), p.5419-5434

2014

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In Vitro Characterization of ETX1317, a Broad-Spectrum β-Lactamase Inhibitor That Restores and Enhances β-Lactam Activity against Multi-Drug-Resistant Enterobacteriales , Including Carbapenem-Resistant Strains

ACS infectious diseases, 2020-06, Vol.6 (6), p.1389-1397

2020

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ESKAPEing the labyrinth of antibacterial discovery

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

In vivo dose response and efficacy of the β-lactamase inhibitor, durlobactam, in combination with sulbactam against the Acinetobacter baumannii-calcoaceticus complex

Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors

N-Hydroxyformamide LpxC inhibitors, their in vivo efficacy in a mouse Escherichia coli infection model, and their safety in a rat hemodynamic assay

Rational design of a new antibiotic class for drug-resistant infections

Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β‑Lactamases

Identification of broad-spectrum antiviral compounds and assessment of the druggability of their target for efficacy against respiratory syncytial virus (RSV)

Antibacterial Drug Discovery: Some Assembly Required

Optimization of Halopemide for Phospholipase D2 inhibition

ETX2514 is a broad-spectrum β-lactamase inhibitor for the treatment of drug-resistant Gram-negative bacteria including Acinetobacter baumannii

Tipranavir (PNU-140690): A Potent, Orally Bioavailable Nonpeptidic HIV Protease Inhibitor of the 5,6-Dihydro-4-hydroxy-2-pyrone Sulfonamide Class

Discovery of Potent, Selective, and Orally Active Carboxylic Acid Based Inhibitors of Matrix Metalloproteinase-13

Identification of Dipeptidyl Nitriles as Potent and Selective Inhibitors of Cathepsin B through Structure-Based Drug Design

Potent and selective 2-naphthylsulfonamide substituted hydroxamic acid inhibitors of matrix metalloproteinase-13

Biophysical Investigation of the Mode of Inhibition of Tetramic Acids, the Allosteric Inhibitors of Undecaprenyl Pyrophosphate Synthase

Challenges and opportunities in the discovery, development, and commercialization of pathogen-targeted antibiotics

Role of the Klebsiella pneumoniae TolC porin in antibiotic efflux

Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases

Pharmacokinetic/Pharmacodynamic Determination and Preclinical Pharmacokinetics of the β-Lactamase Inhibitor ETX1317 and Its Orally Available Prodrug ETX0282

Acinetobacter baumannii OmpA Is a Selective Antibiotic Permeant Porin

Design, Synthesis, and Properties of a Potent Inhibitor of Pseudomonas aeruginosa Deacetylase LpxC

N-Arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B

4‑Aminoquinolone Piperidine Amides: Noncovalent Inhibitors of DprE1 with Long Residence Time and Potent Antimycobacterial Activity

In Vitro Characterization of ETX1317, a Broad-Spectrum β-Lactamase Inhibitor That Restores and Enhances β-Lactam Activity against Multi-Drug-Resistant Enterobacteriales , Including Carbapenem-Resistant Strains

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