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Synthesis and evaluation of vancomycin and vancomycin aglycon analogues that bear modifications in the residue 3 asparagine.

Abstract：

:The synthesis and biological evaluation of a set of residue 3 analogues of vancomycin and its aglycon are described. These investigations follow from the promising biological activity of a protected and synthetically modified vancomycin aglycon analogue in which the asparagine side chain was modified to possess a nitrile, rather than a carboxamide. Although this modification typically was detrimental to antimicrobial activity, hydrophobic vancomycin aglycon analogues that lack a lipid anchor as well as the disaccharide are detailed that exhibit unusual potency against VanB, but not VanA, resistant bacteria.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

McAtee JJ,Castle SL,Jin Q,Boger DL

doi

10.1016/s0960-894x(02)00130-0

subject

Has Abstract

pub_date

2002-05-06 00:00:00

pages

1319-22

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960894X02001300

journal_volume

12

pub_type

杂志文章

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