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In vitro activities of U-100592 and U-100766, novel oxazolidinone antibacterial agents
- G. Zurenko, B. Yagi, S. J. Brickner
- Medicine, BiologyAntimicrobial agents and chemotherapy
- 1 April 1996
Time-kill studies demonstrated a bacteriostatic effect of the analogs against staphylococci and enterococci but a bactericidal effect against streptococci.
Linezolid, the first oxazolidinone antibacterial agent
- K. Leach, S. J. Brickner, M. C. Noe, P. Miller
- Biology, MedicineAnnals of the New York Academy of Sciences
- 1 March 2011
Results have demonstrated that oxazolidinone analogs related to linezolid are effective in treating pulmonary tuberculosis caused by resistant Mycobacterium tuberculosis in animal infection models and suggest additional new therapeutic applications for these antibiotics.
Nonsteroidal anti-inflammatory drug sensitizes Mycobacterium tuberculosis to endogenous and exogenous antimicrobials
- B. Gold, M. Pingle, C. Nathan
- BiologyProceedings of the National Academy of Sciences
- 10 September 2012
A high-throughput screen for compounds that kill Mtb when its replication has been halted by reactive nitrogen intermediates, acid, hypoxia, and a fatty acid carbon source finds modified OPB kills both replicating and NR Mtb and sensitizes both to host-derived and medicinal antimycobacterial agents.
Whole Cell Screen for Inhibitors of pH Homeostasis in Mycobacterium tuberculosis
This approach yields compounds that may lead to the identification of pathways that allow Mtb to survive in acidic environments, a setting in which Mtb is resistant to most of the drugs currently used to treat tuberculosis.
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
- S. J. Brickner, D. Hutchinson, G. Zurenko
- Biology, ChemistryJournal of medicinal chemistry
- 2 February 1996
A novel and practical asymmetric synthesis of (5S)-(acetamidomethyl)-2-oxazolidinones has been developed and is employed for the synthesis of U-100592 and U-100766, which demonstrate potent in vitro activity against Mycobacterium tuberculosis.
Identification of a novel oxazolidinone (U-100480) with potent antimycobacterial activity.
- M. R. Barbachyn, D. Hutchinson, G. Zurenko
- Biology, MedicineJournal of medicinal chemistry
- 2 February 1996
Consideration of these factors, along with a favorable pharmaco-kinetic and chronic toxicity profile in rats, suggests that 6 (U-100480) is a promising antimycobacterial agent.
In vivo activities of U-100592 and U-100766, novel oxazolidinone antimicrobial agents, against experimental bacterial infections
- C. W. Ford, J. C. Hamel, S. J. Brickner
- Biology, MedicineAntimicrobial agents and chemotherapy
- 1 June 1996
The Upjohn oxazolidinones, U-100592 and U-100766, are orally bioavailable synthetic antimicrobial agents with spectra of activity against antibiotic-susceptible and -resistant gram-positive…
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
Addition of PNU-100480 to first-line drugs shortens the time needed to cure murine tuberculosis.
- K. Williams, S. J. Brickner, E. Nuermberger
- Medicine, BiologyAmerican journal of respiratory and critical care…
- 15 August 2009
Results confirm that PNU-100480, which is now in Phase I clinical testing, has sterilizing activity in the murine model and suggest that it may be capable of shortening treatment duration for drug-susceptible as well as drug-resistant tuberculosis in humans.
Piperazinyl oxazolidinone antibacterial agents containing a pyridine, diazene, or triazene heteroaromatic ring.
The antibacterial properties of a series of p Piperazinyl oxazolidinones in which the distal nitrogen of the piperazinyl ring is substituted with a six-membered heteroaromatic ring were evaluated and found to be comparable to that of linezolid.