The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones

…, KC Grega, CS Lee, LA Dolak, EP Seest, W Watt…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 23 p. 4235 - 4239

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Citation Number: 29

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 μg/mL for the most potent congeners). The design, synthesis, antibacterial ...