New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
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.
MicuRx Pharmaceuticals Inc. , Hayward, California 94545, United States.
Mikhail F
MF
Gordeev
Zhengyu Y
ZY
Yuan
D000081:Acetamides / Q000009:adverse effects; D000818:Animals; D000900:Anti-Bacterial Agents / Q000009:adverse effects / Q000737:chemistry* / Q000494:pharmacology; D001854:Bone Marrow Cells / Q000166:cytology / Q000187:drug effects; D017321:Clinical Trials, Phase I as Topic; D015195:Drug Design; D024881:Drug Resistance, Bacterial; D006094:Gram-Positive Bacteria / Q000187:drug effects; D016908:Gram-Positive Bacterial Infections / Q000188:drug therapy; D006801:Humans; D000069349:Linezolid; D008996:Monoamine Oxidase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D023303:Oxazolidinones / Q000009:adverse effects / Q000737:chemistry* / Q000494:pharmacology; D011728:Pyridones / Q000009:adverse effects / Q000737:chemistry* / Q000494:pharmacology; D018805:Sepsis / Q000188:drug therapy
D000081:Acetamides; D000900:Anti-Bacterial Agents; D008996:Monoamine Oxidase Inhibitors; D023303:Oxazolidinones; D011728:Pyridones; C000590780:contezolid; D000069349:Linezolid