312305-94-5Relevant articles and documents
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones
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.
, p. 4235 - 4239 (2007/10/03)
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's0.5 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.