Synthesis and antibacterial evaluation of N-alkyl vancomycins
- PMID: 2921228
- DOI: 10.7164/antibiotics.42.63
Synthesis and antibacterial evaluation of N-alkyl vancomycins
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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