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• W2405699446 abstract "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." @default.
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• W2405699446 date "2015-08-17" @default.
• W2405699446 modified "2023-09-26" @default.
• W2405699446 title "Discovery of a Teraryl Oxazolidinone Compound (<i>S</i>)-<i>N</i>-((3-(3-Fluoro-4-(4-(pyridin-2-yl)-1<i>H</i>-pyrazol-1-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)acetamide Phosphate as a Novel Antimicrobial Agent with Enhanced Safety Profile and Efficacies" @default.
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• W2405699446 doi "https://doi.org/10.1021/acs.jmedchem.5b00152" @default.
• W2405699446 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26212502" @default.
• W2405699446 hasPublicationYear "2015" @default.
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