申请人:Takeda Chemical Industries, Ltd.
公开号:EP0271829A2
公开(公告)日:1988-06-22
compound of the formula
wherein R' and R4 are independently amino or an organic residue bonded through nitrogen, R2 is hydrogen or alkyl which may be substituted, R3 is hydrogen or a protecting group and R5 is hydroxyl which may be substituted or amino which may be substituted or salts thereof; with the proviso that when R1 is amino, sorbylamino or hexanoylamino, R2 is hydrogen or methyl, R4 is amino which may be protected adn R5 is hydroxyl or 2-amidinoethylamino, R3 is a protecting group, and that when R1 is amino, leucylamino, acetylamino or benzyloxycarbonylamino, R3 is hydrogen, methyl or 2-tettrahydropyranyl, R4 is amino, acetylamino or benzyloxycarbonylamino and R5 is hydroxyl which may be substituted or amino which may be substituted, R2 is alkyl which may be substituted, has antibacterial activities against drug-resistant bacteria and therefore can be useful as a chemotherapeutic drug for bacterial infections in mammals.
式中的化合物
其中 R' 和 R4 独立地为氨基或通过氮键合的有机残基,R2 为氢或可被取代的烷基,R3 为氢或保护基团,R5 为可被取代的羟基或可被取代的氨基或其盐;但当 R1 为氨基、山梨氨基或己酰氨基时,R2 为氢或甲基,R4 为可被保护的氨基,R5 为羟基或 2-脒乙基氨基,R3 为保护基;当 R1 为氨基、月桂氨基、乙酰氨基或苄氧羰基氨基时,R3 为氢、甲基或 2-四氢吡喃基、R4 是氨基、乙酰氨基或苄氧羰基氨基,R5 是羟基(可被取代)或氨基(可被取代),R2 是烷基(可被取代)时,具有抗耐药细菌的抗菌活性,因此可用作哺乳动物细菌感染的化疗药物。