SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF NEW TROPONE-SUBSTITUTED PHENYLOXAZOLIDINONE ANTIBACTERIAL AGENTS .2. MODIFICATION OF THE PHENYL RING - THE POTENTIATING EFFECT OF FLUORINE SUBSTITUTION ON IN-VIVO ACTIVITY
Mr. Barbachyn et al., SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF NEW TROPONE-SUBSTITUTED PHENYLOXAZOLIDINONE ANTIBACTERIAL AGENTS .2. MODIFICATION OF THE PHENYL RING - THE POTENTIATING EFFECT OF FLUORINE SUBSTITUTION ON IN-VIVO ACTIVITY, Bioorganic & medicinal chemistry letters, 6(9), 1996, pp. 1009-1014
Various electron-withdrawing groups were incorporated into the meta po
sition of tropone-substituted 3-phenyl-2-oxazolidinones and their infl
uence on antibacterial activity examined. Consideration of in vitro an
d in vivo test results indicated that one or two fluorine atoms flanki
ng the para tropone appendage is the optimum arrangement for these com
pounds. Synthetic routes to enantiomerically enriched analogues are re
ported. (C) 1996 Elsevier Science Ltd.