Author/Authors :
Fred L. Ciske، نويسنده , , Michael R. Barbachyn، نويسنده , , Michael J. Genin، نويسنده , , Kevin C. Grega، نويسنده , , Chi Sing Lee، نويسنده , , Lester A. Dolak، نويسنده , , Eric P. Seest، نويسنده , , William Watt، نويسنده , , Wade J. Adams، نويسنده , , Janice M. Friis، نويسنده , , Charles W. Ford، نويسنده , , Gary E. Zurenko، نويسنده ,
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 MICʹs<0.5 μg/mL for the most potent congeners). The design, synthesis, antibacterial activity and pharmacokinetic profile of a selected series of α-methylated indoline derivatives and a related set of tetrahydroquinolyl and dihydrobenzoxazinyl analogues are discussed.
