Synthesis, crystal structure and biological evaluation of new phosphoramide derivatives as urease inhibitors using docking, QSAR and kinetic studies.
Bisphosphoramide derivatives
Docking
Inhibitory activity
Kinetics
QSAR
Urease enzyme
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
05 2019
05 2019
Historique:
received:
01
11
2018
revised:
20
01
2019
accepted:
27
01
2019
pubmed:
18
2
2019
medline:
14
4
2020
entrez:
18
2
2019
Statut:
ppublish
Résumé
In an attempt to achieve a new class of phosphoramide inhibitors with high potency and resistance to the hydrolysis process against urease enzyme, we synthesized a series of bisphosphoramide derivatives (01-43) and characterized them by various spectroscopic techniques. The crystal structures of compounds 22 and 26 were investigated using X-ray crystallography. The inhibitory activities of the compounds were evaluated against the jack bean urease and were compared to monophosphoramide derivatives and other known standard inhibitors. The compounds containing aromatic amines and their substituted derivatives exhibited very high inhibitory activity in the range of IC
Identifiants
pubmed: 30772649
pii: S0045-2068(18)31251-3
doi: 10.1016/j.bioorg.2019.01.064
pii:
doi:
Substances chimiques
Enzyme Inhibitors
0
Phosphoramides
0
phosphoramide
13597-72-3
Urease
EC 3.5.1.5
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
482-493Informations de copyright
Crown Copyright © 2019. Published by Elsevier Inc. All rights reserved.