194668-50-3Relevant articles and documents
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl- oxazolidinones leading to a promising antibacterial agent
Guo, Bin,Fan, Houxing,Xin, Qisheng,Chu, Wenjing,Wang, Hui,Huang, Yanqin,Chen, Xiaoyan,Yang, Yushe
supporting information, p. 2642 - 2650 (2013/05/09)
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.
AMINOHETEROARYL COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS
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Page/Page column 84, (2010/10/20)
Aminoheteroaryl compounds are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
NOVEL AZA-RING DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS
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Page 16-18, (2008/06/13)
This invention relates to novel aza-dng dedvatives useful as monoamine neurotransmifter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
Heterocyclic compounds useful as pharmaceutical agents
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, (2008/06/13)
Compounds of formula (I) in which all variables are defined in the description and their salts inhibit the enzyme oxido squalene cyclase and are useful in treating hypercholesterolemia and also as anti-fungal agents. Processes for their preparation are also described together with their use in medicine.