Abstract
Oxazolidinones comprise an important class of antibacterial protein synthesis inhibitors. Myelosuppression and monoamine oxidase inhibition (MAOI) are key independent causes for limiting adverse effects in therapy with the sole approved drug of this class, linezolid. This annotation describes a novel oxazolidinone agent, (S)-5-((isoxazol-3-ylamino)methyl)-3-(2,3,5-trifluoro-4-(4-oxo-3,4-dihydropyridin-1(2H)-yl)phenyl)oxazolidin-2-one (MRX-I), distinguished by its high activity against Gram-positive pathogens coupled with markedly reduced potential for myelosuppression and MAOI. The medical need, medicinal chemistry rationale, preclinical data, and phase I clinical trial summary for this new agent are reviewed herein.
MeSH terms
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Acetamides / adverse effects
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Animals
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Anti-Bacterial Agents / adverse effects
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Anti-Bacterial Agents / chemistry*
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Anti-Bacterial Agents / pharmacology
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Bone Marrow Cells / cytology
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Bone Marrow Cells / drug effects
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Clinical Trials, Phase I as Topic
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Drug Design
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Drug Resistance, Bacterial
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Gram-Positive Bacteria / drug effects
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Gram-Positive Bacterial Infections / drug therapy
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Humans
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Linezolid
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Monoamine Oxidase Inhibitors / chemistry
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Monoamine Oxidase Inhibitors / pharmacology
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Oxazolidinones / adverse effects
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Oxazolidinones / chemistry*
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Oxazolidinones / pharmacology
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Pyridones / adverse effects
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Pyridones / chemistry*
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Pyridones / pharmacology
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Sepsis / drug therapy
Substances
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Acetamides
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Anti-Bacterial Agents
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Monoamine Oxidase Inhibitors
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Oxazolidinones
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Pyridones
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contezolid
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Linezolid