The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
SYNTHESIS AND ANTIBACTERIAL EVALUATION OF N-ALKYL VANCOMYCINS
R. NAGARAJANA. A. SCHABELJ. L. OCCOLOWITZF. T. COUNTERJ. L. OTTA. M. FELTY-DUCKWORTH
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1989 Volume 42 Issue 1 Pages 63-72

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Abstract

Over eighty N-alkyl vancomycins were synthesized by reductive alkylation of vancomycin with the appropriate aldehydes. The N-alkyl vancomycins exhibit greater antibacterial activity than the corresponding N-acyl vancomycins and the parent antibiotic. Some of these semisynthetic vancomycins are five times more active than vancomycin. The N-alkyl vancomycins also show longer elimination half-lives in rats than vancomycin.

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© Japan Antibiotics Research Association
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