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zyvox monoamine oxidase

Folkert Reck, Fei Zhou, Marc Girardot, Gunther Kern, Charles J Eyermann, Neil J Hales, Rona R Ramsay, Michael B Gravestock
Oxazolidinones represent a new and promising class of antibacterial agents. Current research in this area is mainly concentrated on improving the safety profile and the antibacterial spectrum. Many oxazolidinones, including linezolid (marketed as Zyvox), are inhibitors of monoamine oxidase A (MAO-A), which presents an undesired side effect. Recently, it was found that the 1,2,3-triazole is a good replacement for the conventional acetamide functionality found in oxazolidinones. We now disclose the finding that 1,2,3-triazoles bearing a substituent like methyl, small substituted methyl, bromo, or a linear (sp-hybridized) group at the 4 position (compounds such as 5, 16, 19, and 21) are good antibacterials with reduced or no activity, within the detection limit of the assay, against MAO-A...
January 27, 2005: Journal of Medicinal Chemistry
Dennis L Stevens, Brian Dotter, Karl Madaras-Kelly
Resistance of Gram-positive bacterial pathogens, such as Staphylococcus aureus and Enterococcus faecium, to existing antibiotics continues to increase, and new antibiotics with activity against these pathogens are in demand. Linezolid (Zyvox, Pharmacia and Upjohn) is the first agent of a new class of antibiotics called the oxazolidinones. Linezolid possesses excellent microbial activity against a wide variety of Gram-positive pathogens including those resistant to methicillin and vancomycin (Vancocin, Eli Lilly)...
February 2004: Expert Review of Anti-infective Therapy
(no author information available yet)
Linezolid (Zyvox--Pharmacia)--the first oxazolidinone antibacterial--is marketed in the UK for treating hospital- and community-acquired pneumonia, skin and soft tissue infections. The manufacturer claims that switching from i.v. to oral administration of linezolid needs no dose adjustment and "will lead to early patient discharge and reduced hospital length of stay" for patients needing treatment for infections caused by Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). Here, we assess the place of linezolid...
July 2001: Drug and Therapeutics Bulletin
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