Basarab, Gregory S. published the artcileDiscovery of Novel DNA Gyrase Inhibiting Spiropyrimidinetriones: Benzisoxazole Fusion with N-Linked Oxazolidinone Substituents Leading to a Clinical Candidate (ETX0914), Safety of (R)-4-Methyloxazolidin-2-one, the main research area is DNA gyrase inhibitor spiropyrimidinetrione benzisoxazole oxazolidinone preparation.
A novel class of bacterial type-II topoisomerase inhibitor displaying a spiropyrimidinetrione architecture fused to a benzisoxazole scaffold shows potent activity against Gram-pos. and fastidious Gram-neg. bacteria. Here, the authors describe a series of N-linked oxazolidinone substituents on the benzisoxazole that improve upon the antibacterial activity of initially described compounds of the class, show favorable PK properties, and demonstrate efficacy in an in vivo Staphylococcus aureus infection model. Inhibition of the topoisomerases DNA gyrase and topoisomerase IV from both Gram-pos. and a Gram-neg. organisms was demonstrated. Compounds showed a clean in vitro toxicity profile, including no genotoxicity and no bone marrow toxicity at the highest evaluated concentrations or other issues that have been problematic for some fluoroquinolones. Compound I was identified for advancement into human clin. trials for treatment of uncomplicated gonorrhea based on a variety of beneficial attributes including the potent activity and the favorable safety profile.
Journal of Medicinal Chemistry published new progress about Antibacterial agents. 4042-43-7 belongs to class oxazolidine, name is (R)-4-Methyloxazolidin-2-one, and the molecular formula is C4H7NO2, Safety of (R)-4-Methyloxazolidin-2-one.
Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem