Sulfonylhydrazones: Design, synthesis and investigation of ectonucleotidase (ALP & e5'NT) inhibition activities.
5'-Nucleotidase
/ antagonists & inhibitors
Alkaline Phosphatase
/ antagonists & inhibitors
Benzopyrans
/ chemical synthesis
Drug Design
Enzyme Inhibitors
/ chemical synthesis
GPI-Linked Proteins
/ antagonists & inhibitors
Humans
Hydrazones
/ chemical synthesis
Molecular Docking Simulation
Structure-Activity Relationship
Sulfinic Acids
/ chemical synthesis
Alkaline phosphatase
Chromen-2-one
Ecto-5ʹ-nucleotidase
Ectonucleotidase inhibitors
Sulfonylhydrazone
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
07 2020
07 2020
Historique:
received:
16
11
2019
revised:
16
03
2020
accepted:
05
04
2020
pubmed:
14
5
2020
medline:
9
3
2021
entrez:
14
5
2020
Statut:
ppublish
Résumé
Medicinal importance of the sulfonylhydrazones is well-evident owing to their binding ability with zinc containing metalloenzymes. In the present study, we have synthesized different series of sulfonylhydrazones by using facile synthetic methods in good to excellent yield. All the successfully prepared sulfonylhydrazones were screened for ectonucleotidase (ALP & e5'NT) inhibitory activity. Among the chromen-2-one scaffold based sulfonylhydrazones, the compounds 7 was found to be most potent inhibitor for h-TNAP (human tissue non-specific alkaline phosphatase) and h-IAP (human intestinal alkaline phosphatase) with IC
Identifiants
pubmed: 32402802
pii: S0045-2068(19)31957-1
doi: 10.1016/j.bioorg.2020.103827
pii:
doi:
Substances chimiques
Benzopyrans
0
Enzyme Inhibitors
0
GPI-Linked Proteins
0
Hydrazones
0
Sulfinic Acids
0
ALPI protein, human
EC 3.1.3.1
ALPL protein, human
EC 3.1.3.1
Alkaline Phosphatase
EC 3.1.3.1
5'-Nucleotidase
EC 3.1.3.5
NT5E protein, human
EC 3.1.3.5
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
103827Informations de copyright
Copyright © 2020 Elsevier Inc. 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.