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Erythromycin a derivative, pharmaceutical composition, antibacterial preparation, process for treating a bacteriologically infectious disease, and use of the erythromycin derivative a or a pharmaceutically acceptable salt thereof.

机译:红霉素衍生物,药物组合物,抗菌制剂,治疗细菌性传染病的方法以及红霉素衍生物a或其药学上可接受的盐的用途。

摘要

"ERYTHROMYCIN A DERIVATIVE, PHARMACEUTICAL COMPOSITION A represented by formula (I): [where n is an integer from 1 to 4, R ^ 1 ^ is a group represented by the formula: a group represented by the formula: a pyridylacetyl group, a 1,2-bis (ethoxycarbonyl) vinyl group, R ^ 2 ^ is the same group as defined for R ^ 1 ^, a hydrogen atom, an alkyl group with 1 to 5 carbon atoms, an alkanoyl group with 2 to 6 carbon atoms or an alkoxycarbonyl group with 2 to 6 carbon atoms, R ^ 1 ^ and R ^ 2 ^ together form a group of formula: = CH-R ^ 14 ^, or R ^ 1 ^ and R ^ 2 ^, together with the nitrogen atom to which they are attached, form a group represented by the formula: R ^ 15 ^ and R ^ 16 ^ are each a hydrogen atom or, when W is a carbon atom, R ^ 15 ^ and R ^ 16 ^, fixed together, form a benzene ring or a naphthalene ring, R ^ 3 ^ is a hydrogen atom, a cinamyl group, R ^ 4 ^ is a hydrogen atom, a group acetyl, a ethylsuccinyl group or a nicotinoil group, A is a group represented by the formula alkyl group with 1 to 5 carbon atoms] or a pharmaceutically acceptable salt thereof, it has a strong antibacterial activity not only against known bacteria sensitive to erythromycin, but also against bacteria resistant to erythromycin.
机译:“式(I)表示的红霉素A衍生物,药物组合物A:[式中,n是1〜4的整数,R ^ 1 ^是下式表示的基团:下式表示的基团:吡啶基乙酰基,a 1,2-双(乙氧羰基)乙烯基,R ^ 2 ^与R ^ 1 ^所定义的基团相同,氢原子,碳数为1至5的烷基,碳数为2至6的烷酰基或具有2至6个碳原子的烷氧羰基,R ^ 1 ^和R ^ 2 ^一起形成下式的基团:= CH-R ^ 14 ^,或R ^ 1 ^和R ^ 2 ^与氮一起与它们连接的原子形成由下式表示的基团:R ^ 15 ^和R ^ 16 ^各自为氢原子,或当W为碳原子时,R ^ 15 ^和R ^ 16 ^固定在一起形成苯环或萘环,R ^ 3 ^为氢原子,肉桂酰基,R ^ 4 ^为氢原子,基团乙酰基,乙基琥珀酰基或烟碱基团,A为下式表示的基团配方醇[具有1至5个碳原子的烷基]或其​​药学上可接受的盐,它不仅对已知对红霉素敏感的细菌具有强的抗菌活性,而且还对对红霉素具有抗性的细菌具有强的抗菌活性。

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