Synthesis and antibacterial activity of new tropone-substituted phenyloxazolidinone antibacterial agents. 1. Identification of leads and importance of the tropone substitution pattern
Incorporation of a substituted tropone moiety into the para position of suitably functionalized 3-phenyl-2-oxazolidinones affords novel and potent antibacterial agents. The effect of the tropone regioisomer and its attendant substituents on antibacterial activity is discussed. Analogues such as 11c and 13b display in vitro and in vivo activity approaching that of the current clinical benchmark, vancomycin.
Barbachyn, Michael R.,Toops, Dana S.,Ulanowicz, Debra A.,Grega, Kevin C.,Brickner, Steven J.,Ford, Charles W.,Zurenko, Gary E.,Hamel, Judith C.,Schaadt, Ronda D.,Stapert, Douglas,Yagi, Betty H.,Buysse, Jerry M.,Demyan, William F.,Kilburn, James O.,Glickman, Suzanne E.