40070-84-6Relevant academic research and scientific papers
Oxazolidinones compound and application thereof
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Paragraph 0144; 0148-0149, (2016/10/10)
The invention provides an oxazolidinones compound shown as the formula VI, or salt, an aquo-complex, or a crystal form of the oxazolidinones compound, which are pharmaceutically acceptable. The invention also provides a preparation method of the compound. In the current field of a chemical drug, activity of most compounds with changed structures becomes better, while toxicity is obviously enhanced, so that the compounds cannot be used as drugs. Compared with a compound in the prior art, the oxazolidinones compound provided in the invention has excellent anti-drug-resistance and antimicrobial activity. What is unexpected is that the oxazolidinones compound has better safety and benefits safe drug use and therapy of a patient.
Discovery of a Teraryl Oxazolidinone Compound (S)-N-((3-(3-Fluoro-4-(4-(pyridin-2-yl)-1H-pyrazol-1-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)acetamide Phosphate as a Novel Antimicrobial Agent with Enhanced Safety Profile and Efficacies
Yang, Tao,Chen, Gong,Sang, Zitai,Liu, Yuanyuan,Yang, Xiaoyan,Chang, Ying,Long, Haiyue,Ang, Wei,Tang, Jianying,Wang, Zhenling,Li, Guobo,Yang, Shengyong,Zhang, Jingren,Wei, Yuquan,Luo, Youfu
, p. 6389 - 6409 (2015/09/07)
A series of novel teraryl oxazolidinone compounds was designed, synthesized, and evaluated for their antimicrobial activity and toxicities. The compounds with aromatic N-heterocyclic substituents at the 4-position of pyrazolyl ring showed better antibacterial activity against the tested bacteria than other compounds with different patterns of substitution. Among all potent compounds, 10f exhibited promising safety profile in MTT assays and in hERG K+ channel inhibition test. Furthermore, its phosphate was found to be highly soluble in water (47.1 mg/mL), which is beneficial for the subsequent in vivo test. In MRSA systemic infection mice models, 10f phosphate exerted significantly improved survival protection compared with linezolid. The compound also demonstrated high oral bioavailability (F = 99.1%). Moreover, from the results of in vivo toxicology experiments, 10f phosphate would be predicted to have less bone marrow suppression (Chemical Equation).
