Thiohydantoins and hydantoins derived from amino acids as potent urease inhibitors: Inhibitory activity and ligand-target interactions.
C. ensiformis
Hydantoins
Molecular docking
NMR
STD
Thiohydantoins
Journal
Chemico-biological interactions
ISSN: 1872-7786
Titre abrégé: Chem Biol Interact
Pays: Ireland
ID NLM: 0227276
Informations de publication
Date de publication:
25 Sep 2022
25 Sep 2022
Historique:
received:
01
03
2022
revised:
10
06
2022
accepted:
13
07
2022
pubmed:
20
7
2022
medline:
11
9
2022
entrez:
19
7
2022
Statut:
ppublish
Résumé
We report the investigation of hydantoins and thiohydantoins derived from L and d-amino acids as inhibitors against the Canavalia ensiformis urease (CEU). The biochemical in vitro assay against CEU revealed a promising inhibitory potential for most thiohydantoins with six of them showing %I higher than the reference inhibitor thiourea (56.5%). In addition, thiohydantoin derived from l-valine, 1b, as well as the hydantoin 2d, derived from l-methionine, were identified as the most potent inhibitors with %I = 90.5 and 85.9 respectively. Enzyme kinetic studies demonstrated a mixed and uncompetitive inhibition profile for these compounds with K
Identifiants
pubmed: 35853540
pii: S0009-2797(22)00250-2
doi: 10.1016/j.cbi.2022.110045
pii:
doi:
Substances chimiques
Amino Acids
0
Enzyme Inhibitors
0
Hydantoins
0
Ligands
0
Thiohydantoins
0
Urease
EC 3.5.1.5
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
110045Informations de copyright
Copyright © 2022 Elsevier B.V. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.