Format

Send to

Choose Destination
See comment in PubMed Commons below
Eur J Med Chem. 2011 May;46(5):1582-92. doi: 10.1016/j.ejmech.2011.02.006. Epub 2011 Mar 5.

Synthesis and biological evaluation of a diazepanone-based library of liposidomycins analogs as MraY inhibitors.

Author information

1
Université Paris Descartes, UMR 8601 CNRS, Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, 45 rue des Saints-Pères, 75006 Paris, France.

Abstract

New inhibitors of the bacterial tranferase MraY are described. A scaffold strategy based on the diazepanone central core of liposidomycins, natural inhibitors of MraY has been developed. It involves the introduction of key structural fragments required for biological activity on enantiopure diazepanones by reductive amination, esterification and glycosylation. Biological evaluation of these compounds on MraY enzyme revealed interesting inhibitory activity for compounds displaying three fragments on the scaffold: a palmitoyl chain, an aminoribose part and an alkyluracil moiety. The inhibitors were also evaluated on MurG enzyme. The best compounds resulted in inhibition with IC50 values in the 100 μM range for one or the other enzyme.

PMID:
21377772
DOI:
10.1016/j.ejmech.2011.02.006
[Indexed for MEDLINE]
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science
    Loading ...
    Support Center