On March 28, 2013, Guo, Bin; Fan, Houxing; Xin, Qisheng; Chu, Wenjing; Wang, Hui; Huang, Yanqin; Chen, Xiaoyan; Yang, Yushe published an article.Application In Synthesis of (R)-5-(Hydroxymethyl)oxazolidin-2-one The title of the article was Solubility-Driven Optimization of (Pyridin-3-yl) Benzoxazinyl-oxazolidinones Leading to a Promising Antibacterial Agent. And the article contained the following:
The solubility-driven structural modification of substituted (pyridin-3-yl)-containing hydrobenzo[b]oxazolo[3,4-d][1,4]oxazinones is described, which resulted in the development of a new series of benzo[b]oxazolo[3,4-d][1,4]oxazinone analogs with high antibacterial activity against Gram-pos. pathogens, including that against linezolid-resistant strains, and low hERG inhibition. With regard to structure-activity relationship (SAR) trends among the various substituents on the pyridyl ring, relatively small and nonbasic substituents were preferable to sterically demanding or basic substituents. Oxazolidinone ring substitution on the pyridyl ring generated analogs with antibacterial activity superior to imidazolidinone ring. Solubility was enhanced by the incorporation of polar groups, especially when compounds were converted to their prodrugs. Among the prodrugs, compound I exhibited excellent solubility and a good pharmacokinetic profile. In a MRSA systemic infection model, compound I displayed an ED50 = 5.00 mg/kg, a potency that is 2-fold better than that of linezolid. The experimental process involved the reaction of (R)-5-(Hydroxymethyl)oxazolidin-2-one(cas: 97859-49-9).Application In Synthesis of (R)-5-(Hydroxymethyl)oxazolidin-2-one
The Article related to oxazolooxazinone pyridyl substituted preparation solubility driven optimization antibacterial activity, antibacterial activity sar gram pos bacteria oxazolooxazinone herg inhibition, sodium phosphate prodrug solubility pharmacokinetic and other aspects.Application In Synthesis of (R)-5-(Hydroxymethyl)oxazolidin-2-one
Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem