Chemical modification of tylosin. Thioether derivatives of tylosin and demycarosyltylosin.

نویسندگان

  • S Omura
  • H Matsubara
  • K Tsuzuki
  • A Nakagawa
چکیده

Thioether derivatives of tylosin and demycarosyltylosin were synthesized by Michael-type addition of thiol to C-11 of the enone moiety on the aglycone. Some of tylosin derivatives were effective to macrolide resistant Staphylococcus aureus, and their in vivo activities were same or superior than that of tylosin.

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منابع مشابه

Chemical modification of tylosin: synthesis of amino derivatives at C-20 position of tylosin and demycarosyltylosin.

Reductive aminations of the aldehyde group at C-20 position of tylosin and demycarosyltylosin (desmycosin) were carried out using primary and secondary amines in the presence of sodium cyanoborohydride. Some of these derivatives brought about higher antimicrobial and ribosome-binding activities, and the structure-activity relationship is discussed.

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A high prevalence of tylosin resistance among Staphylococcus aureus strains isolated from bovine mastitis

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Chemical modification of tylosin.

20-Homo tylosin, 20-nor tylosin, 20-deoxy-19,20-didehydro tylosin (6-vinyl tylosin) and 2",3"-didehydro-3"-deoxy tylosin were prepared by multi-step procedures. 20-Homo tylosin was about twice less active than tylosin while the other compounds exhibited very weak antibacterial activity.

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Physico-chemical properties of new acyl derivatives of tylosin produced by microbial transformation.

By microbial transformation of tylosin (I), the following eight new acyl derivatives were obtained: 3-acetyltylosin (II), 3-propionyltylosin (III), 4"-butyryltylosin (IV), 4"-isovaleryltylosin (V), 3-acetyl-4"-butyryltylosin (VI), 3-acetyl-4"-isovaleryltylosin (VII), 3-propionyl-4"-butyryltylosin (VIII) and 3-propionyl-4"-isovaleryltylosin (IX).

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عنوان ژورنال:
  • The Journal of antibiotics

دوره 37 9  شماره 

صفحات  -

تاریخ انتشار 1984