Structural requirement of tunicamycin V for MraY inhibition.
Anti-Bacterial Agents
/ chemical synthesis
Bacterial Proteins
/ antagonists & inhibitors
Biological Products
/ chemistry
Drug Design
Inhibitory Concentration 50
Staphylococcus aureus
/ enzymology
Transferases
/ antagonists & inhibitors
Transferases (Other Substituted Phosphate Groups)
Tunicamycin
/ chemistry
Antibacterial
Enzyme inhibitor
Natural products
Nucleoside
Structure-activity relationship
Journal
Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298
Informations de publication
Date de publication:
15 04 2019
15 04 2019
Historique:
received:
07
01
2019
revised:
30
01
2019
accepted:
16
02
2019
pubmed:
10
3
2019
medline:
13
3
2020
entrez:
10
3
2019
Statut:
ppublish
Résumé
Elucidating a structure-activity relationship study by evaluating a series of truncated analogues is a simple but important and effective tactic in medicinal chemistry based on natural products with a large and complex chemical structure. In this study, a series of truncated analogues of tunicamycin V were designed and synthesized and their MraY inhibitory activity was investigated in order to gain insight into the effect of these moieties on MraY inhibition.
Identifiants
pubmed: 30850266
pii: S0968-0896(18)31813-3
doi: 10.1016/j.bmc.2019.02.035
pii:
doi:
Substances chimiques
Anti-Bacterial Agents
0
Bacterial Proteins
0
Biological Products
0
Tunicamycin
11089-65-9
Transferases
EC 2.-
Transferases (Other Substituted Phosphate Groups)
EC 2.7.8.-
mraY protein, Bacteria
EC 2.7.8.13
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1714-1719Informations de copyright
Copyright © 2019. Published by Elsevier Ltd.