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

Bypassing Fluoroquinolone Resistance with Quinazolinediones: Studies of Drug–Gyrase–DNA Complexes Having Implications for Drug Design

(2014) Karl Drlica et al.   ACS Chemical Biology

HighIn VitroActivity of the Novel Spiropyrimidinetrione AZD0914, a DNA Gyrase Inhibitor, against Multidrug-Resistant Neisseria gonorrhoeae Isolates Suggests a New Effective Option for Oral Treatment of Gonorrhea

(2014) Susanne Jacobsson et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

In VitroAntibacterial Activity of AZD0914, a New Spiropyrimidinetrione DNA Gyrase/Topoisomerase Inhibitor with Potent Activity against Gram-Positive, Fastidious Gram-Negative, and Atypical Bacteria

(2014) Michael D. Huband et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Characterization of the Novel DNA Gyrase Inhibitor AZD0914: Low Resistance Potential and Lack of Cross-Resistance in Neisseria gonorrhoeae

(2014) Richard A. Alm et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Mechanism of Quinolone Action and Resistance

(2014) Katie J. Aldred et al.   BIOCHEMISTRY

Prioritized Current Unmet Needs for Antibacterial Therapies

(2014) B Spellberg et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Challenges with gonorrhea in the era of multi-drug and extensively drug resistance – are we on the right track?

(2014) Magnus Unemo et al.   Expert Review of Anti-Infective Therapy

Treatment failure with 2 g of azithromycin (extended-release formulation) in gonorrhoea in Japan caused by the international multidrug-resistant ST1407 strain of Neisseria gonorrhoeae

(2014) T. Morita-Ishihara et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Determination of Disk Diffusion and MIC Quality Control Guidelines for GSK2140944, a Novel Bacterial Type II Topoisomerase Inhibitor Antimicrobial Agent

(2014) J. E. Ross et al.   JOURNAL OF CLINICAL MICROBIOLOGY

Novel DNA Gyrase Inhibiting Spiropyrimidinetriones with a Benzisoxazole Scaffold: SAR and in Vivo Characterization

(2014) Gregory S. Basarab et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of a Tetrahydronaphthyridine Spiropyrimidinetrione DNA Gyrase Inhibiting Antibacterial Agent - Differential Substitution at all Five Carbon Atoms of Pyridine.

(2014) Gregory S. Basarab et al.   ORGANIC LETTERS

A New-Class Antibacterial—Almost. Lessons in Drug Discovery and Development: A Critical Analysis of More than 50 Years of Effort toward ATPase Inhibitors of DNA Gyrase and Topoisomerase IV

(2014) Gregory S. Bisacchi et al.   ACS Infectious Diseases

Non-quinolone Inhibitors of Bacterial Type IIA Topoisomerases: A Feat of Bioisosterism

(2013) Claudine Mayer et al.   CHEMICAL REVIEWS

Methicillin-Resistant Staphylococcus aureus Therapy: Past, Present, and Future

(2013) K. A. Rodvold et al.   CLINICAL INFECTIOUS DISEASES

Fragment-to-Hit-to-Lead Discovery of a Novel Pyridylurea Scaffold of ATP Competitive Dual Targeting Type II Topoisomerase Inhibiting Antibacterial Agents

(2013) Gregory S. Basarab et al.   JOURNAL OF MEDICINAL CHEMISTRY

Topoisomerase IV-quinolone interactions are mediated through a water-metal ion bridge: mechanistic basis of quinolone resistance

(2013) Katie J. Aldred et al.   NUCLEIC ACIDS RESEARCH

Trends in antimicrobial resistance inNeisseria gonorrhoeaein the USA: the Gonococcal Isolate Surveillance Project (GISP), January 2006–June 2012

(2013) Robert D Kirkcaldy et al.   SEXUALLY TRANSMITTED INFECTIONS

Bone marrow micronucleus frequencies in the rat after oral administration of cyclophosphamide, hexamethylphosphoramide or gemifloxacin for 2 and 28 days

(2013) Ann T. Doherty et al.   Toxicology Research

Allosteric inhibition of the DNA-dependent ATPase activity of Escherichia coli DNA gyrase by a representative of a novel class of inhibitors

(2012) Adam B. Shapiro et al.   BIOCHEMICAL PHARMACOLOGY

Novel N-Linked Aminopiperidine Inhibitors of Bacterial Topoisomerase Type II with Reduced pKa: Antibacterial Agents with an Improved Safety Profile

(2012) Folkert Reck et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Emerging Threat of Untreatable Gonococcal Infection

(2012) Gail A. Bolan et al.   NEW ENGLAND JOURNAL OF MEDICINE

Antibiotic resistance in Neisseria gonorrhoeae: origin, evolution, and lessons learned for the future

(2011) Magnus Unemo et al.   Annals of the New York Academy of Sciences

Estradiol-Treated Female Mice as Surrogate Hosts for Neisseria gonorrhoeae Genital Tract Infections

(2011) Ann E. Jerse et al.   Frontiers in Microbiology

Pyrazolopyrimidinediones Are Selective Agents for Helicobacter pylori That Suppress Growth through Inhibition of Glutamate Racemase (MurI)

(2009) B. L. M. de Jonge et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Fluoroquinolone-induced immune thrombocytopenia: a report and review

(2009) C. Y. Cheah et al.   INTERNAL MEDICINE JOURNAL

Two cases of failed ceftriaxone treatment in pharyngeal gonorrhoea verified by molecular microbiological methods

(2009) J. Tapsall et al.   JOURNAL OF MEDICAL MICROBIOLOGY

Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success

(2009) Frank Lovering et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of (−)-PNU-286607 by Asymmetric Cyclization of Alkylidene Barbiturates

(2009) J. Craig Ruble et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The Diarylquinoline TMC207 for Multidrug-Resistant Tuberculosis

(2009) Andreas H. Diacon et al.   NEW ENGLAND JOURNAL OF MEDICINE

Discovery and Characterization of QPT-1, the Progenitor of a New Class of Bacterial Topoisomerase Inhibitors

(2008) A. A. Miller et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Mechanism of Action of the Antibiotic NXL101, a Novel Nonfluoroquinolone Inhibitor of Bacterial Type II Topoisomerases

(2008) M. T. Black et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Clerocidin selectively modifies the gyrase-DNA gate to induce irreversible and reversible DNA damage

(2008) X. S. Pan et al.   NUCLEIC ACIDS RESEARCH