The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones |
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Authors: | Ciske Fred L Barbachyn Michael R Genin Michael J Grega Kevin C Lee Chi Sing Dolak Lester A Seest Eric P Watt William Adams Wade J Friis Janice M Ford Charles W Zurenko Gary E |
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Institution: | Pfizer, 7000 Portage Road, Kalamazoo, MI 49001, USA. |
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Abstract: | The oxazolidinones are promising agents for the treatment of infections caused by gram-positive bacteria, including multidrug-resistant strains. In ongoing studies we have discovered that a strategically placed chiral center of appropriate absolute configuration improves the antibacterial activity of indolinyl oxazolidinone analogues (gram-positive MIC's<0.5 microg/mL for the most potent congeners). The design, synthesis, antibacterial activity and pharmacokinetic profile of a selected series of alpha-methylated indoline derivatives and a related set of tetrahydroquinolyl and dihydrobenzoxazinyl analogues are discussed. |
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