Synthesis and antimicrobial evaluation of acyl derivatives of 16-membered macrolide antibiotics related to tylosin
| Autor: | John L. Ott, A. M. Felty-Duckworth, Manuel Debono, Brenda A. Truedell, K. E. Willard, F. T. Counter, Herbert A. Kirst, R. S. Pekarek, John E. Toth |
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| Rok vydání: | 1986 |
| Předmět: |
Pharmacology
chemistry.chemical_classification Bacteria medicine.drug_class Stereochemistry Acylation Aminoglycoside Bacterial Infections Tylosin Antimicrobial Leucomycins Macrolide Antibiotics Bioavailability chemistry.chemical_compound Mice Structure-Activity Relationship chemistry Drug Discovery medicine Structure–activity relationship Animals Lactone |
| Zdroj: | The Journal of antibiotics. 39(8) |
| ISSN: | 0021-8820 |
| Popis: | A large number and wide variety of acyl derivatives of the tylosin-related macrolides 23-demycinosyltylosin (DMT), 23-demycinosyloxytylosin (DMOT) and 5-O-mycaminosyltylonolide (OMT) were synthesized and evaluated. This encompassed conversion of the hydroxyl groups at 2',4' and 23 of the appropriate macrolides to the corresponding esters, in which a variety of different substitution patterns were examined. A wide range of acyl substituents was investigated, particularly for 23-O-acyl derivatives of OMT, since these were substantially more active in vitro than OMT itself. However, the acyl derivatives which were prepared demonstrated no substantial improvement in oral efficacy or bioavailability over the parent macrolides. |
| Databáze: | OpenAIRE |
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