Nagarajan R, Schabel A A, Occolowitz J L, Counter F T, Ott J L, Felty-Duckworth A M
Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285.
J Antibiot (Tokyo). 1989 Jan;42(1):63-72. doi: 10.7164/antibiotics.42.63.
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.
通过用适当的醛对万古霉素进行还原烷基化反应，合成了八十多种N-烷基万古霉素。N-烷基万古霉素比相应的N-酰基万古霉素和母体抗生素表现出更强的抗菌活性。其中一些半合成万古霉素的活性比万古霉素高五倍。N-烷基万古霉素在大鼠体内的消除半衰期也比万古霉素长。
