申请人:FARMITALIA CARLO ERBA S.r.l.
公开号:EP0199490A1
公开(公告)日:1986-10-29
Compounds of the following formula I
wherein X represent a sulphur or an oxygen atom,
R is hydrogen or a C1-C4 alkyl group either unsubstituted or substituted by one or more substituents chosen from a free or protected hydroxy group and halogen atom;
A is a Z, Z-O-CO-or -Z-CO-residue, wherein
Z represents (a) an optionally substituted phenylene or naphthylene group, (b) an optionally substituted heterocyclediyl radical wherein the hetero ring is mono or bicyclic, saturated or unsaturated containing at least one heteroatom selected from the group of oxygen, sulphur and nitrogen;
(c) an optionally substituted linear or branched C,-C7 alkylene radical;
(d) a C2-C4 alkenylene or alkynylene group or a group of formula
or (e) an optionally substituted C3-C8 cycloalkylene ring;
(f) an aralkylene radical of formula
wherein n is 1,2 or 3, and Q(+) represents a
group, wherein
(i) R1, Rz, R3 are independently an optionally substituted alkyl, aralkyl or aryl radical; or
(ii) R, is as defined above under (i) and R2, R3 taken together with the nitrogen atom represent an optionally substituted heterocyclic or fused heterocyclic radical; or
(iii) R,, R2, R3, taken together with the nitrogen atom, represent an optionally substsitut- ed azoniabicyclo or azoniatricyclo radical; or
(iv) R1 R2, R3, taken together with nitrogen atom, represent an optionally substituted pyridinium, pirazinium, pyrazolium, or pyridazinium radical, such radicals being optionally fused with one phenyl ring or with a 5-7 membered, saturated or unsaturated cycloaliphatic or heterocyclic ring, or a pharmaceutically or veterinarily acceptable salt thereof having high antibacterial activity.
下式 I 的化合物
其中 X 代表硫原子或氧原子、
R 是氢或 C1-C4 烷基,可以是未取代的,也可以是被一个或多个取代基取代的 C1-C4 烷基,取代基可选自游离的或受保护的羟基和卤原子;
A 是 Z、Z-O-CO 或 -Z-CO 残基,其中
(a) 任选取代的亚苯基或亚萘基; (b) 任选取代的杂环基,其中杂环为单环或双环,饱和或不饱和,含有至少一个选 自氧、硫和氮组的杂原子;
(c) 任选取代的直链或支链 C,-C7 亚烷基;
(d) 一个 C2-C4 烯基或炔基或一个式基团
(e) 任选取代的 C3-C8 环亚烷基环
(f) 式中的芳烷基
其中 n 为 1、2 或 3,且 Q(+)代表一个
基团,其中
(i) R1、Rz、R3 独立地是任选取代的烷基、芳基或芳基;或
(ii) R 如上文第(i)段所定义,R2、R3 与氮原子一起代表任选取代的杂环或融合杂环基;或
(iii) R、R2、R3 与氮原子一起代表任选取代的偶氮二环或偶氮三环基;或
(iv) R1、R2、R3 与氮原子一起代表任选取代的吡啶鎓、吡嗪鎓、吡唑鎓或哒嗪鎓基,这些基任选与一个苯基环或与一个 5-7 位的饱和或不饱和环脂族或杂环融合,或代表其具有高抗菌活性的药学上或兽医学上可接受的盐。