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    • 3. 发明授权
    • Deformyltylosin derivatives
    • 甲状腺素衍生物
    • US4345069A
    • 1982-08-17
    • US184375
    • 1980-09-05
    • Hideo SakakibaraTatsuro FujiwaraOsamu OkegawaEiichi HondaSusumu WatanabeTetsuo Matsuda
    • Hideo SakakibaraTatsuro FujiwaraOsamu OkegawaEiichi HondaSusumu WatanabeTetsuo Matsuda
    • C07H17/08
    • C07H17/08
    • Deformyltylosin derivatives of the formula ##STR1## wherein A is ##STR2## --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --, R.sub.1 is hydrogen, lower alkanoyl or aryl-lower alkanoyl, X.sub.1 and X.sub.2 are hydrogen or are connected to form a valence bond, Y.sub.1 and Y.sub.2 are hydrogen or are connected to form a valence bond, Q.sub.1 is hydrogen or methyl, Q.sub.2 is hydrogen or ##STR3## R.sub.2 is hydrogen or lower alkanoyl, R is hydrogen or ##STR4## R.sub.3 is hydrogen or C.sub.2-5 alkanoyl, and R.sub.4 is hydrogen or C.sub.2-6 alkanoyl, and when R.sub.3 is not hydrogen, then R.sub.4 is not hydrogen, or a pharmaceutically acceptable salt thereof, have strong antibacterial activities as compared to the known antibiotic tylosin, and also have enhanced antibacterial activities against all macrolide antibiotic-resistant strains such as A, B and C group strains, and have higher blood levels as compared with tylosin.
    • 其中A为-CH = CH-或-CH 2 -CH 2 - ,R 1为氢,低级烷酰基或芳基 - 低级烷酰基,X 1和X 2为氢或连接形成价数的式 键,Y1和Y2是氢或连接形成价键,Q1是氢或甲基,Q2是氢或R2是氢或低级烷酰基,R是氢或者R3是氢或C2-5 烷酰基,R4为氢或C2-6烷酰基,当R3不为氢时,R4为氢,或其药学上可接受的盐与已知抗生素泰乐菌素相比具有较强的抗菌活性,并且还具有增强的抗菌活性 对抗所有大环内酯抗生素抗性菌株如A,B和C组菌株,并且与泰乐菌素相比具有较高的血液水平。