申请人:DAIICHI PHARMACEUTICAL CO., LTD.
公开号:US20040209940A1
公开(公告)日:2004-10-21
This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R
1
is an optionally substituted aromatic group, a salt of the same or a hydrate of both.
1
In the formula, R
2
, R
3
: hydrogen atom, an alkyl group; R
4
, R
5
, R
6
: hydrogen atom, hydroxyl group, a halogen atom, carbamoyl group, an alkyl group, an alkoxyl group, an alkylthio group; R
7
, R
8
: hydrogen atom, an alkyl group; R
9
: an alkyl group, an alkenyl group, a halogenoalkyl group, a cyclic alkyl group, an aryl group, a heteroaryl group, an alkoxyl group having from 1 to 6 carbon atoms, an alkylamino group; R
10
:hydrogen atom, an alkylthio group; R
11
: hydrogen atom, amino group, hydroxyl group, thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; X
1
: halogen atom, a hydrogen atom; A
1
: nitrogen atom, C-X
2
; X
2
: hydrogen atom, amino group, a halogen atom, cyano group, an halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; A
2
, A
3
:>C═C (-A
1
═)—N(—R
9
)—, >N—C (-A
1
>)═C(—R
9
)—; R
10
and R
9
or R
9
and X
2
may be integrated to for a ring structure; and Y: hydrogen atom, ester forming group.
本发明提供了一种喹诺酮衍生物,其具有强效的抗菌活性,可用于治疗包括耐药菌株在内的各种细菌感染。该化合物的结构式如下:其中R1为可选的取代芳基,其盐或水合物。在公式中,R2、R3:氢原子、烷基;R4、R5、R6:氢原子、羟基、卤素原子、氨基甲酰基、烷基、烷氧基、烷硫基;R7、R8:氢原子、烷基;R9:烷基、烯基、卤代烷基、环烷基、芳基、杂环芳基、含有1~6个碳原子的烷氧基、烷基氨基;R10:氢原子、烷硫基;R11:氢原子、氨基、羟基、硫醇基、卤代甲基基、烷基、烯基、炔基、烷氧基;X1:卤素原子、氢原子;A1:氮原子、C-X2;X2:氢原子、氨基、卤素原子、氰基、卤代甲基基、卤代甲氧基基、烷基、烯基、炔基、烷氧基;A2、A3:>C=C(-A1H)-N(-R9)-、>N-C(-A1>)=CH(-R9)-;R10和R9或R9和X2可以结合形成环状结构;Y:氢原子、酯形成基。