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  • Title: Preparation and evaluation of 3,4''-ester derivatives of 16-membered macrolide antibiotics related to tylosin.
    Author: Kirst HA, Debono M, Willard KE, Truedell BA, Toth JE, Turner JR, Berry DR, Briggs BB, Fukuda DS, Daupert VM.
    Journal: J Antibiot (Tokyo); 1986 Dec; 39(12):1724-35. PubMed ID: 3818446.
    Abstract:
    A large group of ester derivatives of tylosin-related macrolides was prepared in which the hydroxyl groups at C-3 and C-4'' were acylated by either chemical or biochemical methods. Most of the derivatives exhibited excellent in vitro antimicrobial activity. However, only the 3,4''-diacyl derivatives of tylosin and macrocin showed any significant improvements of in vivo efficacy against experimental infections in rodents.
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