申请人:ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
公开号:EP0825194A2
公开(公告)日:1998-02-25
A novel amide derivative of amythiamicin is now provided, which is represented by the general formula (I)
wherein n is an integer of 1 to 6, R1 is a hydrogen atom, a carboxyl group or a hydroxylmethyl group, and R2 is a group of the formula -COOR3 where R3 is a hydrogen atom or a lower alkyl group or a benzyl group optionally substituted by a halogen or a hydroxyl group, or R2 is a group of the formula -NR4R5 where R4 is a hydrogen atom or a lower alkyl group and R5 is a hydrogen atom, a lower alkyl group, 3-aminopropyl group, 3-[2-(p-chloro or bromophenyl)ethyl]aminopropyl group or 3-(n-butylamino)propyl group, or R2 is a methyl group, a hydroxyl group or a guanidino group of the formula -NH-C(=NH)-NH2, or a pharmaceutically acceptable salt or ester thereof. These compounds of the formula (I) exhibit useful antibacterial activities and are soluble in water, and some of them are found to exhibit an excellent antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA).
现提供一种新型的氨基硫胺酰胺衍生物,其通式为(I)
其中 n 为 1 至 6 的整数,R1 为氢原子、羧基或羟甲基,R2 为式 -COOR3 的基团,其中 R3 为氢原子或低级烷基或任选被卤素或羟基取代的苄基,或 R2 为式 -NR4R5 的基团,其中 R4 为氢原子或低级烷基,R5 为氢原子、低级烷基、3-氨基丙基、3-[2-(对氯或溴苯基)乙基]氨基丙基或 3-(正丁氨基)丙基,或 R2 为甲基、羟基或式 -NH-C(=NH)-NH2 的胍基,或其药学上可接受的盐或酯。这些式(I)化合物表现出有用的抗菌活性,并可溶于水,其中一些对耐甲氧西林金黄色葡萄球菌(MRSA)表现出优异的抗菌活性。