申请人:PFIZER INC.
公开号:EP0413455A2
公开(公告)日:1991-02-20
Quinolone carboxylic acids 7-substituted by azabicyclo groups have antibacterial activity.
Antibacterial
wherein
R¹ is hydrogen, a pharmaceutically acceptable cation, or alkyl;
Y, when taken independently, is ethyl, t-butyl, vinyl, cyclopropyl, 2-fluoroethyl, p-fluorophenyl, or o,p-difluorophenyl;
W is hydrogen, F, Cl, Br, alkyl, alkoxy, NH₂, NHCH₃;
A is CH, CF, CCl, COCH₃, C-CH₃, C-CN or N; or
A is carbon and is taken together with Y and the carbon and nitrogen to which A and Y are attached to form a five or six membered ring which may contain oxygen or a double bond, and which may have attached thereto R⁸ which is methyl or methylene; and
R² is
wherein R³, R⁴, R⁵, R⁶, R⁷, R⁹, R¹⁰ and R²⁵ are each independently H, CH₃, CH₂NH₂, CH₂NHCH₃ or CH₂NHC₂H₅, and R⁵, R⁶, R⁷, and R⁹ may also independently be NH₂, NHCH₃ or NHC₂H₅.
氮杂双环基团取代的 7-喹啉酮羧酸具有抗菌活性。
抗菌剂
其中
R¹ 是氢、药学上可接受的阳离子或烷基;
Y 独立存在时为乙基、叔丁基、乙烯基、环丙基、2-氟乙基、对氟苯基或 o,p-二氟苯基;
W 是氢、F、Cl、Br、烷基、烷氧基、NH₂、NHCH₃;
A 是 CH、CF、CCl、COCH₃、C-CH₃、C-CN 或 N;或
A 是碳,与 Y 以及 A 和 Y 所连接的碳和氮共同形成一个五或六成员环,该环可能含有氧或双键,其上可能连接有甲基或亚甲基的 R⁸;以及
R² 是
其中 R³、R⁴、R⁵、R⁶、R⁷、R⁹、R¹⁰ 和 R²⁵ 各自独立地为 H、CH₃、CH₂NH₂、CH₂HCH₃ 或 CH₂NHC₂H₅,以及 R⁵、R⁶、R⁷ 和 R⁹ 也可以独立地为 NH₂、NHCH₃ 或 NHC₂H₅。