- Efficient and stereoselective one-pot synthesis of benzo[b] oxazolo[3,4- d] [1,4]oxazin-1-ones
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An efficient and mild one-pot convergent synthesis protocol has been developed for benzo[b]oxazolo[3,4-d][1,4]oxazin-1-one derivatives through the Mitsunobu reaction and sequential cyclization. Various tricyclic fused benzoxazinyl-oxazolidinones (20 examp
- Cheng, Shihao,Huang, Haihong,Lu, Haijia,Zhang, Dongfeng,Zhao, Hongyi,Zhao, Wenting
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- BENZOXAZINE OXAZOLIDINONE COMPOUND, PREPARATION METHOD AND APPLICATION THEREOF
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Disclosed are a benzoxazine oxazolidinone compound shown by a general formula (I), an optical isomer thereof or a pharmaceutically acceptable salt thereof, a preparation method thereof, and an application thereof in preparing a drug for treating an infectious disease and in particular, an infectious disease caused by multidrug resistant bacteria.
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Paragraph 0024; 0025
(2016/01/26)
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- Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl- oxazolidinones leading to a promising antibacterial agent
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The solubility-driven structural modification of (pyridin-3-yl) benzoxazinyl-oxazolidinones is described, which resulted in the development of a new series of benzoxazinyl-oxazolidinone analogues with high antibacterial activity against Gram-positive 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 analogues 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 85 exhibited excellent solubility and a good pharmacokinetic profile. In a MRSA systemic infection model, compound 85 displayed an ED 50 = 5.00 mg/kg, a potency that is 2-fold better than that of linezolid.
- Guo, Bin,Fan, Houxing,Xin, Qisheng,Chu, Wenjing,Wang, Hui,Huang, Yanqin,Chen, Xiaoyan,Yang, Yushe
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p. 2642 - 2650
(2013/05/09)
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