Chemical modification of tylosin.
نویسندگان
چکیده
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.
منابع مشابه
Chemical modification of tylosin. Thioether derivatives of tylosin and demycarosyltylosin.
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.
متن کاملChemical 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.
متن کاملA high prevalence of tylosin resistance among Staphylococcus aureus strains isolated from bovine mastitis
The macrolides appear to have considerable effects for treatment of bovine mastitis because of excellent diffusion into the mammary gland, long half-life, low protein binding, high intracellular concentration and lipid solubility. Acquired resistance to macrolides in Staphylococcus aureus is primarily related to target-site modification through acquisition of an erm gene. In t...
متن کاملFermentation-derived compounds as a source of new products
New products may be sought by modifying older fermentation products, exemplified by the semisynthetic antibiotic tilmicosin and other derivatives of tylosin. Another approach is to screen fermentation broths, exemplified by the discovery of the structurally-unique insecticidal macrolide spinosad. The polyketide class of fermentation products encompasses a wide diversity of chemical structures a...
متن کاملPhysico-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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ورودعنوان ژورنال:
- The Journal of antibiotics
دوره 48 7 شماره
صفحات -
تاریخ انتشار 1995