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糖肽类抗生素的还原烷基化：合成与抗菌活性

Reductive alkylation of glycopeptide antibiotics: synthesis and antibacterial activity.

作者信息

Cooper R D, Snyder N J, Zweifel M J, Staszak M A, Wilkie S C, Nicas T I, Mullen D L, Butler T F, Rodriguez M J, Huff B E, Thompson R C

机构信息

Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA.

出版信息

J Antibiot (Tokyo). 1996 Jun;49(6):575-81. doi: 10.7164/antibiotics.49.575.

DOI:10.7164/antibiotics.49.575
PMID:8698642
Abstract

Reductive alkylation of the A82846 family of glycopeptide antibiotics has the potential of producing seven products. N-Alkylation of the disaccharide amino function can be accomplished selectively, and offers the greatest increase in antibacterial activity. Products resulting from N-alkylation of LY264826 (A82846B) provide the most potent derivatives as compared to other members of this class of antibiotics. Two of these derivatives, LY307599 and LY333328 are approximately 500 times more active than vancomycin against vancomycin-resistant enterococci.

摘要

糖肽类抗生素A82846家族的还原烷基化有产生七种产物的可能性。二糖氨基官能团的N-烷基化可以选择性地实现，并且能使抗菌活性得到最大程度的提高。与这类抗生素的其他成员相比，LY264826（A82846B）的N-烷基化产物是最有效的衍生物。其中两种衍生物，LY307599和LY333328对耐万古霉素肠球菌的活性比万古霉素高约500倍。

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