1. Synthesis and antibacterial activity of derivatives of the glycopeptide antibiotic A-40926 and its aglycone.
- Author
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Hermann R, Ripamonti F, Romanò G, Restelli E, Ferrari P, Goldstein BP, Berti M, and Ciabatti R
- Subjects
- Animals, Anti-Bacterial Agents chemistry, Escherichia coli drug effects, Esters, Haemophilus influenzae drug effects, Mice, Microbial Sensitivity Tests, Molecular Structure, Structure-Activity Relationship, Teicoplanin analogs & derivatives, Anti-Bacterial Agents chemical synthesis, Anti-Bacterial Agents pharmacology, Glycopeptides, Gram-Negative Bacteria drug effects, Gram-Positive Cocci drug effects, Neisseria gonorrhoeae drug effects
- Abstract
Starting from the antibiotic A-40926 and the aglycone of A-40926 a series of compounds were prepared by modifying the free functionalities. Their antimicrobial activity was determined, particularly against Neisseria gonorrhoeae, against which A-40926, unlike other natural glycopeptides, is active. Improved in vivo activity was displayed by the monomethyl ester of A-40926 esterified at the carboxyl group of the N-acylamino-glucuronyl moiety.
- Published
- 1996
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