Synthesis and Evaluation of N -Phenylpyrrolamides as DNA Gyrase B Inhibitors

Discovery and development of kibdelomycin, a new class of broad-spectrum antibiotics targeting the clinically proven bacterial type II topoisomerase

(2016) Sheo B. Singh   BIOORGANIC & MEDICINAL CHEMISTRY

A Gestalt approach to Gram-negative entry

(2016) Lynn L. Silver   BIOORGANIC & MEDICINAL CHEMISTRY

Fragment-based discovery of DNA gyrase inhibitors targeting the ATPase subunit of GyrB

(2016) Michael F. Mesleh et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

New N -phenyl-4,5-dibromopyrrolamides and N -Phenylindolamides as ATPase inhibitors of DNA gyrase

(2016) Nace Zidar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Antibacterial drug discovery in the resistance era

(2016) Eric D. Brown et al.   NATURE

Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design

(2016) Jason B. Cross et al.   ACS Medicinal Chemistry Letters

The Whys and Wherefores of Antibiotic Resistance

(2016) Cameron R. Strachan et al.   Cold Spring Harbor Perspectives in Medicine

Topoisomerase Inhibitors: Fluoroquinolone Mechanisms of Action and Resistance

(2016) David C. Hooper et al.   Cold Spring Harbor Perspectives in Medicine

N-Phenyl-4,5-dibromopyrrolamides and N-Phenylindolamides as ATP Competitive DNA Gyrase B Inhibitors: Design, Synthesis, and Evaluation

(2015) Nace Zidar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 4,5,6,7-Tetrahydrobenzo[1,2-d]thiazoles as Novel DNA Gyrase Inhibitors Targeting the ATP-Binding Site

(2015) Tihomir Tomašič et al.   JOURNAL OF MEDICINAL CHEMISTRY

ESKAPEing the labyrinth of antibacterial discovery

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

Prospects for Developing New Antibacterials Targeting Bacterial Type IIA Topoisomerases

(2014) Tihomir Tomašić et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Optimization of Pyrrolamide Topoisomerase II Inhibitors Toward Identification of an Antibacterial Clinical Candidate (AZD5099)

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

Second-Generation Antibacterial Benzimidazole Ureas: Discovery of a Preclinical Candidate with Reduced Metabolic Liability

(2014) Anne-Laure Grillot et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

The FDA Reboot of Antibiotic Development

(2013) David M. Shlaes et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

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

(2013) Claudine Mayer et al.   CHEMICAL REVIEWS

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

Tricyclic GyrB/ParE (TriBE) Inhibitors: A New Class of Broad-Spectrum Dual-Targeting Antibacterial Agents

(2013) Leslie W. Tari et al.   PLoS One

Pyrrolopyrimidine inhibitors of DNA gyrase B (GyrB) and topoisomerase IV (ParE). Part I: Structure guided discovery and optimization of dual targeting agents with potent, broad-spectrum enzymatic activity

(2012) Leslie W. Tari et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Pyrrolopyrimidine inhibitors of DNA gyrase B (GyrB) and topoisomerase IV (ParE), Part II: Development of inhibitors with broad spectrum, Gram-negative antibacterial activity

(2012) Micheal Trzoss et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel DNA gyrase inhibitors: Microbiological characterisation of pyrrolamides

(2012) Maria Uria-Nickelsen et al.   INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

Structure-Based Discovery of Substituted 4,5′-Bithiazoles as Novel DNA Gyrase Inhibitors

(2012) Matjaž Brvar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pyrrolamide DNA Gyrase Inhibitors: Fragment-Based Nuclear Magnetic Resonance Screening To Identify Antibacterial Agents

(2011) Ann E. Eakin et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Pyrrolamide DNA gyrase inhibitors: Optimization of antibacterial activity and efficacy

(2011) Brian A. Sherer et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of Kibdelomycin, A Potent New Class of Bacterial Type II Topoisomerase Inhibitor by Chemical-Genetic Profiling in Staphylococcus aureus

(2011) John W. Phillips et al.   CHEMISTRY & BIOLOGY

Challenges of Antibacterial Discovery

(2011) L. L. Silver   CLINICAL MICROBIOLOGY REVIEWS

Inhibition of DNA gyrase and DNA topoisomerase IV of Staphylococcus aureus and Escherichia coli by aminocoumarin antibiotics

(2011) S. Alt et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Novel Dual-Targeting Benzimidazole Urea Inhibitors of DNA Gyrase and Topoisomerase IV Possessing Potent Antibacterial Activity: Intelligent Design and Evolution through the Judicious Use of Structure-Guided Design and Stucture−Activity Relationships

(2008) Paul S. Charifson et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Scalable Synthesis of MN-447, an Antagonist for Integrins αvβ3and αIIbβ3

(2008) Minoru Ishikawa et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT