申请人:——
公开号:US20040102433A1
公开(公告)日:2004-05-27
1. A &bgr;-lactam compound of the formula [1];
1
wherein R
1
is a lower alkyl, a lower alkyl substituted by a hydroxy; R
2
is a hydrogen, a lower alkyl; X is O, S, NH; m and n are 0 to 4, Y
1
is a halogen, cyano, a hydroxy, an amino, a lower alkyloxy, a lower alkylamino, a carboxy, a carbamoyl, a lower alkyl, etc., Y
2
is hydrogen, an alkyl, cyano, —C(R
3
)═NR
4
(wherein R
3
and R
4
are hydrogen, an amino, an alkyl, etc., or R
3
and R
4
may combine each other together with the nitrogen atom to form a 5- to 7-membered heterocyclic group), or a pharmaceutically acceptable salt thereof, or a non-toxic ester thereof, which has an excellent antibacterial activity against Gram-positive bacteria, especially against MRSA and MRCNS.
一种化学式为[1]的A &bgr;-内酰胺化合物,其中R1是低碳基,被羟基取代的低碳基; R2是氢,低碳基; X是O,S,NH; m和n为0至4,Y1是卤素,氰基,羟基,氨基,低碳基氧基,低碳基氨基,羧基,氨基甲酰基,低碳基等,Y2是氢,烷基,氰基,—C(R3)═NR4(其中R3和R4是氢,氨基,烷基等,或R3和R4可以相互结合形成5-至7成员杂环基的氮原子),或其药学上可接受的盐,或其非毒性酯,对革兰氏阳性菌,特别是对MRSA和MRCNS具有出色的抗菌活性。