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J Antibiot (Tokyo). 1989 Jan;42(1):63-72.

Synthesis and antibacterial evaluation of N-alkyl vancomycins.

Author information

1
Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285.

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.

PMID:
2921228
DOI:
10.7164/antibiotics.42.63
[Indexed for MEDLINE]
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