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19544365783
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Most of the oxazolidinones reported by Upjohn/Pharmacia to have superior safety profiles in a 30-day rat toxicity model have donating nitrogens in the para-position of the phenyl group. These agents include linezolid, eperezolid, U-100480 (thiomorpholine), and U-97456 (indoline). See Ref. 1. DuPont agents DuP-721 and DuP-105 lacking a para-amine functionality had more severe toxicity in a 30-day rat model (in house data)
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Ihara Chem Ind Co Ltd; Japan Patent, JP-04244067, 92-337745, 1992
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19544370434
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note
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2). The MIC was defined as the lowest drug concentration that prevented physical growth
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22
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0026532148
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C.H. Park, D.R. Brittelli, C.L.J. Wang, F.D. Marsh, W.A. Gregory, M.A. Wuonola, R.J. McRipley, V.S. Eberly, A.M. Slee, and M. Forbes J. Med. Chem. 35 1992 1156 1165
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Eberly, V.S.8
Slee, A.M.9
Forbes, M.10
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23
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19544373186
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note
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The MIC of 25 against Streptococcus pneumoniae A9585 is actually quite impressive, but this determination was not repeated. Also, compound 25 had MIC's of 8 μg/mL against two other strains (S. pneumoniae A27881 and S. pneumoniae A28272) not included in Table 1
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25
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19544379600
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note
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Staphylococcus aureus/Pen+ A15090, Inoculum 1.05 × 107 cfu/mouse ip in 7% mucin, drugs dissolved in 10% DMSO, 5% Tw-80, and water, administered orally b.i.d., 1 and 5 h post infection, death recorded for 8 days, 10 mice per group
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26
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19544376724
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note
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1H NMR and LC/MS)
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