The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Reductive Alkylation of Glycopeptide Antibiotics: Synthesis and Antibacterial Activity
ROBIN D. G. COOPER, NANCY J. SNYDER, MARK J. ZWEIFEL, MICHAEL A. STASZAK, STEPHEN C. WILKIE, THALIA I. NICAS, DEBORAH L. MULLEN, THOMAS F. BUTLER, MICHAEL J. RODRIGUEZ, BRET E. HUFF, RICHARD C. THOMPSON
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JOURNAL FREE ACCESS

1996 Volume 49 Issue 6 Pages 575-581

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Abstract

Reductive alkylation of the A82846 family of glycopeptide antibiotics has the potential of producing seven products. N-Alkylation of the disaccharide amino function can be accomplished selectively, and offers the greatest increase in antibacterial activity. Products resulting from N-alkylation of LY264826 (A82846B) provide the most potent derivatives as compared to other members of this class of antibiotics. Two of these derivatives, LY307599 and LY333328 are approximately 500 times more active than vancomycin against vancomycin-resistant enterococci.

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© Japan Antibiotics Research Association
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The Journal of Antibiotics, Series A

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