| 摘要 |
PCT No. PCT/US94/08904 Sec. 371 Date Mar. 5, 1996 Sec. 102(e) Date Mar. 5, 1996 PCT Filed Aug. 16, 1994 PCT Pub. No. WO95/07271 PCT Pub. Date Mar. 16, 1995A compound of structural Formula I: <IMAGE>erein: X is O, S, SO, SO2, SNR10 or S(O)NR10; R is (a) hydrogen, (b) C1-C8 alkyl optionally substituted with one or more of the following: F, Cl, hydroxy, C1-C8 alkoxy, C1 -C8 acyloxy or -O-CH2-Ph, (c) C3-C6 cycloalkyl, (d) amino, (e) C1-C8 alkylamino, (f) C1-C8 dialkylamino or (g) C1-C8 alkoxy; R1 is H, except when X is O then R1 can be H, CH3, CN, CO2H, CO2R or (CH2)mR11 (m is 1 or 2); R2 is independently H, F or Cl; R3 is H except when X is O and R1 is CH3 then R3 can be H or CH3; R10 is independently H, C1-C4 alkyl (optionally substituted with chloro, fluoro, hydroxy, C1-C8 alkoxy, amino, C1-C8 alkylamino, or C1-C8 dialkylamino) or p-toluenesulfonyl; R11 is hydrogen, OH, OR, OCOR, NH2, NHCOR or N(R10)2; and n is 0, 1 or 2. The oxazine and thiazine oxazolidinone derivatives are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
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