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Synthesis and biological evaluation of a diazepanone-based library of liposidomycins analogs as MraY inhibitors.
Synthesis and biological evaluation of a diazepanone-based library of liposidomycins analogs as MraY inhibitors.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2011 May; Vol. 46 (5), pp. 1582-92. Date of Electronic Publication: 2011 Mar 05. - Publication Year :
- 2011
-
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.<br /> (Copyright © 2011 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Aminoglycosides chemical synthesis
Aminoglycosides chemistry
Dose-Response Relationship, Drug
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Molecular Structure
Small Molecule Libraries
Stereoisomerism
Structure-Activity Relationship
Transferases (Other Substituted Phosphate Groups)
Aminoglycosides pharmacology
Azepines chemistry
Bacterial Proteins antagonists & inhibitors
Enzyme Inhibitors chemical synthesis
Transferases antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 46
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 21377772
- Full Text :
- https://doi.org/10.1016/j.ejmech.2011.02.006