New carbon-linked azole oxazolidinones with improved potency and pharmacokinetics |
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| Authors: | Hauck Sheila I Cederberg Christer Doucette Amanda Grosser Lena Hales Neil J Poon Grace Gravestock Michael B |
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| Affiliation: | AstraZeneca R&D Boston, Infection Discovery, 35 Gatehouse Park, Waltham, MA 02451, USA. Sheila.Hauck@astrazeneca.com |
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| Abstract: | Substitution of phenyl oxazolidinones with carbon-linked azoles resulted in the discovery of a new class of potent oxazolidinones that have excellent Gram-positive activity. In addition, replacement of the C-5 acetamide side chains with a 4-methyl triazole diminished monoamine oxidase activity. The synthesis and biological evaluation of these compounds are reported. |
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