Discovery of Novel DNA Gyrase Inhibiting Spiropyrimidinetriones: Benzisoxazole Fusion with N-Linked Oxazolidinone Substituents Leading to a Clinical Candidate (ETX0914) was written by Basarab, Gregory S.;Doig, Peter;Galullo, Vincent;Kern, Gunther;Kimzey, Amy;Kutschke, Amy;Newman, Joseph P.;Morningstar, Marshall;Mueller, John;Otterson, Linda;Vishwanathan, Karthick;Zhou, Fei;Gowravaram, Madhusudhan. And the article was included in Journal of Medicinal Chemistry in 2015.SDS of cas: 97859-51-3 This article mentions the following:
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. In the experiment, the researchers used many compounds, for example, (S)-5-(Hydroxymethyl)oxazolidin-2-one (cas: 97859-51-3SDS of cas: 97859-51-3).
(S)-5-(Hydroxymethyl)oxazolidin-2-one (cas: 97859-51-3) belongs to oxazolidine derivatives. Oxazolidine-based compounds have started to attract attention also in the medicinal and materials chemistry fields. Oxazolidines are commonly used as metal ligands in asymmetric catalysis, synthetic intermediates in organic synthesis, and also used as the protecting groups.SDS of cas: 97859-51-3
Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem