Synthesis, biological evaluation and molecular docking of novel pyrazole derivatives as potent carbonic anhydrase and acetylcholinesterase inhibitors.
Acetylcholinesterase
/ metabolism
Animals
Carbonic Anhydrase I
/ antagonists & inhibitors
Carbonic Anhydrase II
/ antagonists & inhibitors
Carbonic Anhydrase Inhibitors
/ chemical synthesis
Cholinesterase Inhibitors
/ chemical synthesis
Dose-Response Relationship, Drug
Electrophorus
Humans
Molecular Docking Simulation
Molecular Structure
Pyrazoles
/ chemical synthesis
Structure-Activity Relationship
Acetylcholinesterase
Carbonic anhydrase
Enzyme inhibition
Substituted pyrazole
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:
05
12
2018
revised:
02
02
2019
accepted:
04
02
2019
pubmed:
16
2
2019
medline:
14
4
2020
entrez:
16
2
2019
Statut:
ppublish
Résumé
A series of substituted pyrazole compounds (1-8 and 9a, b) were synthesized and their structure was characterized by IR, NMR, and Mass analysis. These obtained novel pyrazole derivatives (1-8 and 9a, b) were emerged as effective inhibitors of the cytosolic carbonic anhydrase I and II isoforms (hCA I and II) and acetylcholinesterase (AChE) enzymes with K
Identifiants
pubmed: 30769267
pii: S0045-2068(18)31420-2
doi: 10.1016/j.bioorg.2019.02.013
pii:
doi:
Substances chimiques
Carbonic Anhydrase Inhibitors
0
Cholinesterase Inhibitors
0
Pyrazoles
0
pyrazole
3QD5KJZ7ZJ
Acetylcholinesterase
EC 3.1.1.7
Carbonic Anhydrase I
EC 4.2.1.-
Carbonic Anhydrase II
EC 4.2.1.-
CA2 protein, human
EC 4.2.1.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
420-427Informations de copyright
Copyright © 2019. Published by Elsevier Inc.