申请人:Pharmacia & Upjohn Company
公开号:US05652238A1
公开(公告)日:1997-07-29
A compound of structural Formula (I) or pharmaceutically acceptable salts thereof wherein: R is --C(O)--R.sup.1, --PO.sub.3 .dbd. or --P(O)(OH).sub.2 ; R.sup.1 is C.sub.1-6 alkyl, --N(R.sup.4).sub.2, C.sub.1-6 alkyl-N(R.sup.4).sub.2, --phenyl--N(R.sup.4).sub.2, --phenyl-NHC(O)CH.sub.2 NH.sub.2, --C.sub.2 H.sub.4 -morpholinyl, pyridinyl, C.sub.1-6 alkyl-OH, C.sub.1-6 alkyl-OCH.sub.3, C.sub.1-6 alkyl C(O)CH.sub.3, --O--C.sub.1-6 alkyl-OCH.sub.3, C.sub.0-3 alkyl-piperazinyl (optionally substituted with C.sub.1-3 alkyl), imidazolyl, C.sub.1-6 alkyl-COOH, --C(CH.sub.2 OH).sub.2 CH.sub.3 ; R.sup.2 and R.sup.3 are independently selected from hydrogen or F except at least one of R.sup.2 or R.sup.3 is F; R.sup.4 are independently selected from hydrogen or C.sub.1-6 alkyl. The compounds are water soluble and are useful antimicrobial agents, effective against a number of human veterinary pathogens, including multiply-resistant staphylococci, enterococci and streptococci, as well as anerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis.
结构式(I)的化合物或其药用盐,其中:R为--C(O)--R.sup.1,--PO.sub.3 .dbd.或--P(O)(OH).sub.2;R.sup.1为C.sub.1-6烷基,--N(R.sup.4).sub.2,C.sub.1-6烷基-N(R.sup.4).sub.2,--苯基--N(R.sup.4).sub.2,--苯基-NHC(O)CH.sub.2 NH.sub.2,--C.sub.2 H.sub.4 -吗啉基,吡啶基,C.sub.1-6烷基-OH,C.sub.1-6烷基-OCH.sub.3,C.sub.1-6烷基C(O)CH.sub.3,--O--C.sub.1-6烷基-OCH.sub.3,C.sub.0-3烷基-哌嗪基(可选择性地取代为C.sub.1-3烷基),咪唑基,C.sub.1-6烷基-COOH,--C(CH.sub.2 OH).sub.2 CH.sub.3;R.sup.2和R.sup.3分别选择自氢或F,除非R.sup.2或R.sup.3中至少有一个为F;R.sup.4独立选择自氢或C.sub.1-6烷基。这些化合物可溶于水,是有用的抗菌剂,对多种人兽共患病原体具有有效作用,包括多重耐药葡萄球菌、肠球菌和链球菌,以及厌氧生物如拟杆菌和梭菌属,以及耐酸生物如结核分枝杆菌。