Publications and Presentations

Publications

• Zhou, J., Bhattacharjee, A., Chen, S., Chen, Y. et al. Design at the atomic level: generation of novel hybrid biaryloxazolidinones as promising new antibiotics. 2008. Bioorganic & Medicinal Chemistry Letters 18: 6179 — 6183.
• Zhou, J., Bhattacharjee, A., Chen, S., Chen, Y. et al. Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics. 2008. Bioorganic & Medicinal Chemistry Letters 18: 6175 — 6178.
• Skripkin, E., McConnell, T.S., DeVito, J., Lawrence, L., Ippolito, J.A., Duffy, E.M., Sutcliffe, J., Franceschi, F. Rχ-01, a new family of oxazolidinones that overcome ribosome-based linezolid resistance. 2008. Antimicrobial Agents and Chemotherapy 52: 3550 — 3557.
• Ippolito, J.A., Kanyo, Z.F., Wang, D., Franceschi, F., Moore, P.B., Steitz, T.A., Duffy, E.M. Crystal structure of the oxazolidinone antibiotic linezolid bound to the 50S ribosomal subunit. 2008. Journal of Medicinal Chemistry 51: 3353 — 3356.
• Lawrence L., Danese, P., DeVito, J., Franceschi, F., Sutcliffe, J. In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens. 2008. Antimicrobial Agents and Chemotherapy 52: 1653 — 1662.

Posters and Presentations

ICAAC 2011

• Postantibiotic Effect of Radezolid against Eight Staphylococci (0.18mb)

ECCMID 2011

• Potency of radezolid (RX-1741) and torezolid (DA-7157) tested against a collection of linezolid-non-susceptible strains with genetically defined resistance mechanisms (0.19mb)

ICAAC 2010

• A1-015-Evaluation of Radezolid Against a Methicillin-resistant Staphylococccus aureus Rat Granuloma Pouch Infection (1.82mb)
• B-2020-Anti-tuberculosis Activity of Radezolid (2.00mb)
• C1-095-Radezolid Overcomes cfr-mediated Linezolid-resistance by Efficiently Inhibiting Protein Synthesis in cfr-methylated Ribosomes (2.16mb)

ICAAC 2009

• A1-1938 Radezolid, A Novel Oxazolidinone, Accumulates in Infected Thigh Tissue (1.86mb)
• E-810 In Vitro Activity of Radezolid against MRSA Causing Skin and Wound Infections from the United States, Europe, and Asia (0.64mb)

ICAAC 2008

• A Phase 2 Study Comparing Two Doses of Radezolid to Linezolid in adults with uSSSIs
  (1.94mb)

ICAAC 2005

• A Computational Suite for the Discovery of Designer Oxazolidinones Suitable for IV and Oral Usage (3.04mb)
• The Pharmacokinetics of Designer Oxazolidinones in Sprague-Dawley Rats (0.40mb)
• In Vivo Efficacy of Designer Oxazolidinones in Murine Infectious Models (7.27mb)
• Resistance Studies on Designer Oxazolidinones (0.19mb)
• Anti-anaerobic Activity of Designer Oxazolidinones Compared with Those of Clindamycin (Clin), Metronidazole (Met), Linezolid (Lin), and Levofloxacin (Lev) (0.51mb)
• In Vitro Activity of Designer Oxazolidinones against Gram-positive Hospital Pathogens
  (0.60mb)
• In Vitro Activity of Designer Oxazolidinones against Respiratory Pathogens (0.52mb)
• Designer Oxazolidinones Bind to the 50S Peptidyl-Transferase Region and Can Overcome Ribosome-Based Linezolid Resistance (0.83mb)
• Structural Basis for the Binding of RX-01, a Novel Oxazolidinone Class, to Bacterial Ribosomes (2.44mb)
• Structure-Based Design and Synthesis of Novel Amino Acid Amide-Oxazolidinones (2.53mb)
• Design at the atomic level- Synthesis of biaryl Oxazolidinones as Potent, Orally Active Antibiotics (0.65mb)

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Posters and Presentations

ICAAC 2011

• Crystallographic evidence that TAN-1057 and the blasticidin S family of antibiotics inhibit translation by stabilizing a distorted binding mode of P-site tRNA (0.95mb)
• Structural Basis for the Binding of RX-04, a Novel Broad Spectrum Antibacterial Class, to Bacterial Ribosomes (0.92mb)
• The Molecular Tuning of RX-04, a NovelBroad Spectrum Antibacterial Class, for Coverage of MDR Gram-negative Pathogens (0.75mb)
• Completely Novel Antibiotics for Treating Multidrug-resistant Gram-negative Infections: the Isocytosines (0.59mb)
• Completely Novel Antibiotics for Treating Multidrug-resistant Gram-negative Infections: the Phenoxazinocytosines (0.79mb)
• Completely Novel Antibiotics for Treating Multidrug-resistant Gram-negative Infections: The Pyrrolocytosines (0.56mb)
• In vitro Activity of Novel Protein Synthesis Inhibitors Against Gram-Positive Pathogens
  (0.21mb)
• In vitro Antibacterial Activity of Novel Protein Synthesis Inhibitors Against Enterobacteriaceae (0.24mb)
• Novel Protein Synthesis Inhibitors Demonstrating in vitro Antibacterial Activity Against Acinetobacter baumannii and Pseudomonas aeruginosa (0.22mb)
• In Vitro Evaluation of Rib-X Novel Compounds' Potency against Selected Isolates of Pseudomonas Aeruginosa (0.51mb)
• Antimicrobial Activity and Spectrum of compounds from the RX-04 class of Novel Protein Synthesis Inhibitors (0.23mb)
• Novel Ribosome Inhibitors are Efficacious in a Murine Peritonitis Model Caused by Different Bacterial Pathogens (0.48mb)
• Novel Ribosome Inhibitors are Efficacious in a Murine Kidney Infection Model Caused by Staphylococcus aureus MRSA USA300 (0.20mb)
• Novel Ribosome Inhibitors are Efficacious in a Murine Skin and Soft Tissue Infection Model Caused by Klebsiella pneumoniae (0.19mb)

ECCMID 2011

• Completely novel protein synthesis inhibitors demonstrate efficacy in three mouse models of infection (1.07mb)
• Antimicrobial activity of a novel program of protein synthesis inhibitors against clinical isolates containing KPC and NDM-1 carbapenemases (2.03mb)
• Determination of the mechanism of action of three novel chemical scaffolds with broad-spectrum antibacterial activity, including multidrug-resistant Gram-negative pathogens
  (1.99mb)
• Three completely novel antibiotic scaffolds for treating multidrug-resistant Gram-negative infections (1.76mb)

ICAAC 2009

• F2-861 Novel Antibiotic Classes to Treat Gram-negative Infections (2.00mb)

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Publications

• Hanselmann,R., Job, G.E., Johnson, G., Lou, R. et al. Synthesis of an Antibacterial Compound Containing a 1,4-Substituted 1H-1,2,3-Triazole: A Scaleable Alternative to the 'Click' Reaction. 2010. Organic Process Research & Development 14: 152 — 158.
• DeVito, J.A. Recombineering with tolC as a selectable/counter-selectable marker: remodeling the rRNA operons of Escherichia coli. 2008. Nucleic Acids Research 36: e4.
• Franceschi, F., Duffy, E.M.Structure-based drug design meets the ribosome. 2006. Biochemical Pharmacology 71: 1016 — 1025.
• Sutcliffe, J.A. Improving on nature: antibiotics that target the ribosome. 2005. Current Opinions in Microbiology 8: 534 — 542.
• Franceschi, F., Kanyo, Z., Sherer E.C., Sutcliffe, J. Macrolide resistance from the ribosome perspective. 2004. Current Drug Targets &mdash Infectious Disorders 4: 177 — 191.

Posters and Presentations

ICAAC 2010

• C1-666-Crystal Structures of the Glutarimide Antibiotics Cycloheximide Bound to the E-site of the Large Ribosomal Subunit (2.45mb)
• F1-2153-Ribosomal Target Modifications Designed to Evaluate the Potency of Enhanced Macrolides (2.14mb)
• F2-867-Structure-based Design of a New Class of Biaryl Florfenicol Antibiotics (2.81mb)

Ribosomes 2010

• Enhanced Macrolides: Overcoming Resistance with a Novel Mechanism of Action (1.54mb)

ICAAC 2009

• F1-2050 Enhanced Macrolides: Overcoming Resistance by Improving Target Affinity (1.53mb)
• F1-2049 Enhanced Macrolides- Optimized Molecular Properties for Oral Exposure (2.03mb)

Gordon Research Conferences 2008

• Structure-Based Drug DesignTargeting Infectious Disease Overcoming Resistance and Extending the Antimicrobial Spectrum of Macrolide Antibiotics (0.57mb)
• Structure-Based Drug Design Targeting Infectious Diseases (1.06mb)

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