4-Oxycoumarinyl linked acetohydrazide Schiff bases as potent urease inhibitors.
Chromene/coumarin
In silico
In vitro
Structure-activity relationship
Synthesis
Urease inhibitory activity
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
12 2020
12 2020
Historique:
received:
04
07
2020
revised:
07
09
2020
accepted:
08
10
2020
pubmed:
23
10
2020
medline:
17
6
2021
entrez:
22
10
2020
Statut:
ppublish
Résumé
Urease enzyme is responsible to catalyze the hydrolysis of urea into carbamate and ammonia. Then carbamate hydrolyzed to ammonia and carbon dioxide. Excess release of ammonia leads to increase pH in stomach that actually encourages the survival of Helicobacter pylori. H. pylori involves in various disorders most commonly peptic ulcer, pyelonephritis, hepatic coma, kidney stone formation, urolithiasis, and encephalopathy. Apart from many pharmacological properties, coumarin and Schiff bases are known to possess urease inhibitory activity. Therefore, these two pharmacologically important scaffolds are combined into single hybrid molecules to assess their potential as urease inhibitors. For this aim, N'-benzylidene-2-((2-oxo-2H-chromen-4-yl)oxy)acetohydrazide Schiff base derivatives 3-27 were synthesized by following a three step reaction strategy. Structures of all synthetic molecules were characterized by EI-MS,
Identifiants
pubmed: 33091669
pii: S0045-2068(20)31663-1
doi: 10.1016/j.bioorg.2020.104365
pii:
doi:
Substances chimiques
Coumarins
0
Enzyme Inhibitors
0
Hydrazines
0
Schiff Bases
0
Urease
EC 3.5.1.5
acetylhydrazine
SK0DPC9098
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
104365Informations de copyright
Copyright © 2020 Elsevier Inc. All rights reserved.