Antibiotics in the clinical pipeline in 2011

Challenges of Antibacterial Discovery

(2011) L. L. Silver   CLINICAL MICROBIOLOGY REVIEWS

Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent

(2011) Weon Bin Im et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The challenge of new drug discovery for tuberculosis

(2011) Anil Koul et al.   NATURE

A guiding hand for antibiotics

(2011) Dan Jones   NATURE REVIEWS DRUG DISCOVERY

Clostridium difficile: progress and challenges

(2010) John G. Bartlett   Annals of the New York Academy of Sciences

Challenges of antibacterial discovery revisited

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

Phase 2, Randomized, Double-Blind, Dose-Ranging Study Evaluating the Safety, Tolerability, Population Pharmacokinetics, and Efficacy of Oral Torezolid Phosphate in Patients with Complicated Skin and Skin Structure Infections

(2010) P. Prokocimer et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Cellular Pharmacokinetics of the Novel Biaryloxazolidinone Radezolid in Phagocytic Cells: Studies with Macrophages and Polymorphonuclear Neutrophils

(2010) S. Lemaire et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Cellular Pharmacodynamics of the Novel Biaryloxazolidinone Radezolid: Studies with Infected Phagocytic and Nonphagocytic cells, Using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila

(2010) S. Lemaire et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

In Vitro Antibacterial Activities of JNJ-Q2, a New Broad-Spectrum Fluoroquinolone

(2010) B. J. Morrow et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Activity of the Investigational Fluoroquinolone Finafloxacin against Ciprofloxacin-Sensitive and -Resistant Acinetobacter baumannii Isolates

(2010) P. G. Higgins et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Comparative In Vitro Activities of Nemonoxacin (TG-873870), a Novel Nonfluorinated Quinolone, and Other Quinolones against Clinical Isolates

(2010) T.-L. Lauderdale et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

CEM-101 Activity against Gram-Positive Organisms

(2010) L. N. Woosley et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Comparative In Vitro Antimicrobial Activities of Torezolid (TR-700), the Active Moiety of a New Oxazolidinone, Torezolid Phosphate (TR-701), Determination of Tentative Disk Diffusion Interpretive Criteria, and Quality Control Ranges

(2010) S. D. Brown et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Investigation of the Potential for Mutational Resistance to XF-73, Retapamulin, Mupirocin, Fusidic Acid, Daptomycin, and Vancomycin in Methicillin-ResistantStaphylococcus aureusIsolates during a 55-Passage Study

(2010) David J. Farrell et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Pharmacokinetics and Safety of CXA-101, a New Antipseudomonal Cephalosporin, in Healthy Adult Male and Female Subjects Receiving Single- and Multiple-Dose Intravenous Infusions

(2010) Y. Ge et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

PA-824 Exhibits Time-Dependent Activity in a Murine Model of Tuberculosis

(2010) Zahoor Ahmad et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Oritavancin Disrupts Membrane Integrity of Staphylococcus aureus and Vancomycin-Resistant Enterococci To Effect Rapid Bacterial Killing

(2010) A. Belley et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

In Vitro Properties of BAL30072, a Novel Siderophore Sulfactam with Activity against Multiresistant Gram-Negative Bacilli

(2010) M. G. P. Page et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Synthesis and Spectrum of the Neoglycoside ACHN-490

(2010) J. B. Aggen et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Contrasting Effects of Acidic pH on the Extracellular and Intracellular Activities of the Anti-Gram-Positive Fluoroquinolones Moxifloxacin and Delafloxacin againstStaphylococcus aureus

(2010) Sandrine Lemaire et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Improved production of A40926 by Nonomuraea sp. through deletion of a pathway-specific acetyltransferase

(2010) Margherita Sosio et al.   APPLIED MICROBIOLOGY AND BIOTECHNOLOGY

A Phase II Study of Antofloxacin Hydrochloride, a Novel Fluoroquinolone, for the Treatment of Acute Bacterial Infections

(2010) Jin Wang et al.   CHEMOTHERAPY

The 10 × ‘20 Initiative: Pursuing a Global Commitment to Develop 10 New Antibacterial Drugs by 2020

(2010)   CLINICAL INFECTIOUS DISEASES

Challenges in Anti‐Infective Development in the Era of Bad Bugs, No Drugs: A Regulatory Perspective Using the Example of Bloodstream Infection as an Indication

(2010) Helen W. Boucher   CLINICAL INFECTIOUS DISEASES

Combating evolution with intelligent design: the neoglycoside ACHN-490

(2010) Eliana S Armstrong et al.   CURRENT OPINION IN MICROBIOLOGY

The transcription inhibitor lipiarmycin blocks DNA fitting into the RNA polymerase catalytic site

(2010) Audrey Tupin et al.   EMBO JOURNAL

New antibiotics for selective treatment of gastrointestinal infection caused byClostridium difficile

(2010) Alan P Johnson   EXPERT OPINION ON THERAPEUTIC PATENTS

The nitroimidazooxazines (PA-824 and analogs): structure–activity relationship and mechanistic studies

(2010) William A Denny et al.   Future Medicinal Chemistry

Oritavancin: a novel lipoglycopeptide active against Gram-positive pathogens including multiresistant strains

(2010) Emilio Bouza et al.   INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

DNA gyrase and topoisomerase IV are dual targets of zabofloxacin in Streptococcus pneumoniae

(2010) Hee Soo Park et al.   INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

In vitro activity of XF-73, a novel antibacterial agent, against antibiotic-sensitive and -resistant Gram-positive and Gram-negative bacterial species

(2010) David J. Farrell et al.   INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

Discovering new antimicrobial agents

(2010) Robert C. Moellering   INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

Antimicrobial characterisation of solithromycin (CEM-101), a novel fluoroketolide: activity against staphylococci and enterococci

(2010) Shannon D. Putnam et al.   INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

The emergence of ‘hypervirulence’ in Clostridium difficile

(2010) Stephen T. Cartman et al.   INTERNATIONAL JOURNAL OF MEDICAL MICROBIOLOGY

Antibacterial activity of finafloxacin under different pH conditions against isogenic strains of Escherichia coli expressing combinations of defined mechanisms of fluoroquinolone resistance

(2010) Nadine-C. Emrich et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

The problem of complicated skin and skin structure infections: the need for new agents

(2010) R. C. Moellering   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

N-chlorotaurine, a natural antiseptic with outstanding tolerability

(2010) W. Gottardi et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Pharmacokinetics and Whole‐Blood Bactericidal Activity againstMycobacterium tuberculosisof Single Doses of PNU‐100480 in Healthy Volunteers

(2010) Robert S. Wallis et al.   JOURNAL OF INFECTIOUS DISEASES

Triclosan - an update

(2010) S. Saleh et al.   LETTERS IN APPLIED MICROBIOLOGY

The antibacterial lead discovery challenge

(2010)   NATURE REVIEWS DRUG DISCOVERY

The antibiotics market

(2010) Bashar Hamad   NATURE REVIEWS DRUG DISCOVERY

Cethromycin: A Promising New Ketolide Antibiotic for Respiratory Infections

(2010) Sally Rafie et al.   PHARMACOTHERAPY

Pharmacokinetics of antofloxacin hydrochloride, a novel fluoroquinolone, after single-dose intravenous administration in healthy Chinese male volunteers

(2010) J. Wang et al.   XENOBIOTICA

De Novo Design of Antimicrobial Polymers, Foldamers, and Small Molecules: From Discovery to Practical Applications

(2009) Gregory N. Tew et al.   ACCOUNTS OF CHEMICAL RESEARCH

Iclaprim, a Novel Diaminopyrimidine for the Treatment of Resistant Gram-Positive Infections

(2009) Carrie A Sincak et al.   ANNALS OF PHARMACOTHERAPY

Multicenter, Randomized Study of the Efficacy and Safety of Intravenous Iclaprim in Complicated Skin and Skin Structure Infections

(2009) D. Krievins et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

In Vivo Characterization of the Peptide Deformylase Inhibitor LBM415 in Murine Infection Models

(2009) C. S. Osborne et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

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

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

Safety, Tolerability, and Pharmacokinetics of PA-824 in Healthy Subjects

(2009) A. M. Ginsberg et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Multiple-Dose Safety, Tolerability, and Pharmacokinetics of Oral Nemonoxacin (TG-873870) in Healthy Volunteers

(2009) D. T. Chung et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Dose Escalation Study of the Safety, Tolerability, and Pharmacokinetics of Nemonoxacin (TG-873870), a Novel Potent Broad-Spectrum Nonfluorinated Quinolone, in Healthy Volunteers

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

Activities of Dalbavancin against a Worldwide Collection of 81,673 Gram-Positive Bacterial Isolates

(2009) D. J. Biedenbach et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

In Vitro Activity of NXL104 in Combination with  -Lactams against Klebsiella pneumoniae Isolates Producing KPC Carbapenemases

(2009) A. Endimiani et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

In Vitro Activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with Defined Macrolide Resistance Mechanisms

(2009) P. McGhee et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Stieglitz rearrangement of N,N-dichloro-β,β-disubstituted taurines under mild aqueous conditions

(2009) Timothy P. Shiau et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Quaternary ammonium N,N-dichloroamines as topical, antimicrobial agents

(2009) Charles Francavilla et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

CEM-101, a novel fluoroketolide: antimicrobial activity against a diverse collection of Gram-positive and Gram-negative bacteria

(2009) Shannon D. Putnam et al.   DIAGNOSTIC MICROBIOLOGY AND INFECTIOUS DISEASE

Amadacycline

(2009) Y. Wang et al.   DRUGS OF THE FUTURE

Nemonoxacin

(2009) A. Arjona et al.   DRUGS OF THE FUTURE

Peptide deformylase – a promising therapeutic target for tuberculosis and antibacterial drug discovery

(2009) Anshika Sharma et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

XF-73, a novel antistaphylococcal membrane-active agent with rapid bactericidal activity

(2009) N. Ooi et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

XF-70 and XF-73, novel antibacterial agents active against slow-growing and non-dividing cultures of Staphylococcus aureus including biofilms

(2009) N. Ooi et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Activity of the siderophore monobactam BAL30072 against multiresistant non-fermenters

(2009) S. Mushtaq et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Has the era of untreatable infections arrived?

(2009) D. M. Livermore   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Crystal Structures of the Human and Fungal Cytosolic Leucyl-tRNA Synthetase Editing Domains: A Structural Basis for the Rational Design of Antifungal Benzoxaboroles

(2009) Elena Seiradake et al.   JOURNAL OF MOLECULAR BIOLOGY

Public–private partnership tackles TB challenges in parallel

(2009) Sarah Webb   NATURE REVIEWS DRUG DISCOVERY

The Diarylquinoline TMC207 for Multidrug-Resistant Tuberculosis

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

A Comparative Review of the Lipoglycopeptides: Oritavancin, Dalbavancin, and Telavancin

(2009) Michael T Guskey et al.   PHARMACOTHERAPY

A crystal structure of a dimer of the antibiotic ramoplanin illustrates membrane positioning and a potential Lipid II docking interface

(2009) J. B. Hamburger et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

De novo design and in vivo activity of conformationally restrained antimicrobial arylamide foldamers

(2009) S. Choi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Inhibitors of FabI, an Enzyme Drug Target in the Bacterial Fatty Acid Biosynthesis Pathway

(2008) Hao Lu et al.   ACCOUNTS OF CHEMICAL RESEARCH

Selectivity of TMC207 towards Mycobacterial ATP Synthase Compared with That towards the Eukaryotic Homologue

(2008) A. C. Haagsma et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

R -01, a New Family of Oxazolidinones That Overcome Ribosome-Based Linezolid Resistance

(2008) E. Skripkin et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Promising Antituberculosis Activity of the Oxazolidinone PNU-100480 Relative to That of Linezolid in a Murine Model

(2008) K. N. Williams et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Clinical Outcomes, Safety, and Pharmacokinetics of OPT-80 in a Phase 2 Trial with Patients with Clostridium difficile Infection

(2008) T. Louie et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Early Bactericidal Activity and Pharmacokinetics of the Diarylquinoline TMC207 in Treatment of Pulmonary Tuberculosis

(2008) R. Rustomjee et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Mechanism and Inhibition of saFabI, the Enoyl Reductase fromStaphylococcus aureus†

(2008) Hua Xu et al.   BIOCHEMISTRY

Design at the atomic level: Design of biaryloxazolidinones as potent orally active antibiotics

(2008) Jiacheng Zhou et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and SAR of novel parenteral anti-pseudomonal cephalosporins: Discovery of FR264205

(2008) Ayako Toda et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Bad Bugs, No Drugs: No ESKAPE! An Update from the Infectious Diseases Society of America

(2008) Helen W. Boucher et al.   CLINICAL INFECTIOUS DISEASES

Ketolides – The Modern Relatives of Macrolides

(2008) Markus Zeitlinger et al.   CLINICAL PHARMACOKINETICS

Zabofloxacin (DW-224a) activity against Neisseria gonorrhoeae including quinolone-resistant strains

(2008) Ronald N. Jones et al.   DIAGNOSTIC MICROBIOLOGY AND INFECTIOUS DISEASE

Whither antibacterial drug discovery?

(2008) Steven J. Projan   DRUG DISCOVERY TODAY

Are natural products still the best source for antibacterial discovery? The bacterial entry factor

(2008) Lynn L Silver   Expert Opinion on Drug Discovery

Use of cethromycin, a new ketolide, for treatment of community-acquired respiratory infections

(2008) Margaret R Hammerschlag et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

What is in the pipeline for Gram-negative pathogens?

(2008) George H Talbot   Expert Review of Anti-Infective Therapy

New antibiotic agents for bloodstream infections

(2008) Paschalis I. Vergidis et al.   INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

Lipiarmycin targets RNA polymerase and has good activity against multidrug-resistant strains of Mycobacterium tuberculosis

(2008) M. Kurabachew et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Diarylquinolines Are Bactericidal for Dormant Mycobacteria as a Result of Disturbed ATP Homeostasis

(2008) Anil Koul et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

PA-824 Kills Nonreplicating Mycobacterium tuberculosis by Intracellular NO Release

(2008) R. Singh et al.   SCIENCE

Synthesis development of an aminomethylcycline antibiotic via an electronically tuned acyliminium Friedel–Crafts reaction

(2008) John Y.L. Chung et al.   TETRAHEDRON LETTERS

N-Chloro-2,2-dimethyltaurines: a new class of remarkably stable N-chlorotaurines

(2008) Lu Wang et al.   TETRAHEDRON LETTERS

Pharmacodynamics and pharmacokinetics of SQ109, a new diamine-based antitubercular drug

(2004) Lee Jia et al.   BRITISH JOURNAL OF PHARMACOLOGY