title: 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.
authors.affiliation: Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285.
authors.forename: R
authors.initials: R
authors.lastname: Nagarajan
authors.forename: A A
authors.initials: AA
authors.lastname: Schabel
authors.forename: J L
authors.initials: JL
authors.lastname: Occolowitz
authors.forename: F T
authors.initials: FT
authors.lastname: Counter
authors.forename: J L
authors.initials: JL
authors.lastname: Ott
authors.forename: A M
authors.initials: AM
authors.lastname: Felty-Duckworth
mesh_terms: D000818:Animals; D051381:Rats; D013329:Structure-Activity Relationship; D014640:Vancomycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D014640:Vancomycin