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Preparation and evaluation of 3,4'-ester derivatives of 16-membered macrolide antibiotics related to tylosin |
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| Authors: | H A Kirst M Debono K E Willard B A Truedell J E Toth J R Turner D R Berry B B Briggs D S Fukuda V M Daupert |
| 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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