Synthesis, biological evaluation and in silico studies of novel N-substituted phthalazine sulfonamide compounds as potent carbonic anhydrase and acetylcholinesterase inhibitors.
Acetylcholinesterase
/ metabolism
Animals
Carbonic Anhydrase Inhibitors
/ chemical synthesis
Carbonic Anhydrases
/ isolation & purification
Cholinesterase Inhibitors
/ chemical synthesis
Dose-Response Relationship, Drug
Electrophorus
Humans
Isoenzymes
/ antagonists & inhibitors
Molecular Docking Simulation
Molecular Structure
Phthalazines
/ chemical synthesis
Structure-Activity Relationship
Sulfonamides
/ chemical synthesis
Acetylcholinesterase
Carbonic anhydrase
Enzyme inhibitors
Molecular docking
Phthalazine
Sulfonamide
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
08 2019
08 2019
Historique:
received:
27
04
2019
revised:
15
05
2019
accepted:
19
05
2019
pubmed:
28
5
2019
medline:
23
9
2020
entrez:
27
5
2019
Statut:
ppublish
Résumé
The synthesis, characterization and biological evaluation of a series of novel N-substituted phthalazine sulfonamide (5a-l) are disclosed. Phthalazines which are nitrogen-containing heterocyclic compounds are biologically preferential scaffolds, endowed with versatile pharmacological activity, such as anti-inflammatory, cardiotonic vasorelaxant, anticonvulsant, antihypertensive, antibacterial, anti-cancer action. The compounds were investigated for the inhibition against the cytosolic hCA I, II and AChE. Most screened sulfonamides showed high potency in inhibiting hCA II, widely involved in glaucoma, epilepsy, edema, and other pathologies (K
Identifiants
pubmed: 31129502
pii: S0045-2068(19)30667-4
doi: 10.1016/j.bioorg.2019.103004
pii:
doi:
Substances chimiques
Carbonic Anhydrase Inhibitors
0
Cholinesterase Inhibitors
0
Isoenzymes
0
Phthalazines
0
Sulfonamides
0
Acetylcholinesterase
EC 3.1.1.7
Carbonic Anhydrases
EC 4.2.1.1
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
103004Informations de copyright
Copyright © 2019 Elsevier Inc. All rights reserved.