Deep eutectic solvent mediated synthesis of 3,4-dihydropyrimidin-2(1H)-ones and evaluation of biological activities targeting neurodegenerative disorders.
Acetylcholinesterase
/ metabolism
Cholinesterase Inhibitors
/ chemical synthesis
Deep Eutectic Solvents
/ chemistry
Dose-Response Relationship, Drug
Humans
Molecular Docking Simulation
Molecular Structure
Monoamine Oxidase
/ metabolism
Monoamine Oxidase Inhibitors
/ chemical synthesis
Neurodegenerative Diseases
/ drug therapy
Neuroprotective Agents
/ chemical synthesis
Pyrimidinones
/ chemical synthesis
Structure-Activity Relationship
Deep Eutectic Solvent
Dihydropyrimidinones
Ectonucleotidase inhibitors
Ionic Liquids
Response surface method
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
01 2022
01 2022
Historique:
received:
30
05
2021
revised:
19
10
2021
accepted:
25
10
2021
pubmed:
20
11
2021
medline:
14
1
2022
entrez:
19
11
2021
Statut:
ppublish
Résumé
Substitution of hazardous and often harmful organic solvents with "green" and "sustainable" alternative reaction media is always desirous. Ionic liquids (IL) have emerged as valuable and versatile liquids that can replace most organic solvents in a variety of syntheses. However, recently new types of low melting mixtures termed as Deep Eutectic Solvents (DES) have been utilized in organic syntheses. DES are non-volatile in nature, have sufficient thermal stability, and also have the ability to be recycled and reused. Hence DES have been used as alternative reaction media to perform different organic reactions. The availability of green, inexpensive and easy to handle alternative solvents for organic synthesis is still scarce, hence our interest in DES mediated syntheses. Herein we have investigated Biginelli reaction in different DES for the synthesis of 3,4-dihydropyrimidin-2(1H)-ones. Monoamine oxidases and cholinesterases are important drug targets for the treatment of various neurological disorders such as Alzheimer's disease, Parkinson's disease, depression and anxiety. The compounds synthesized herein were evaluated for their inhibitory potential against these enzymes. Some of the compounds were found to be highly potent and selective inhibitors. Compounds 1 h and 1c were the most active monoamine oxidase A (MAO A) (IC
Identifiants
pubmed: 34798458
pii: S0045-2068(21)00834-8
doi: 10.1016/j.bioorg.2021.105457
pii:
doi:
Substances chimiques
Cholinesterase Inhibitors
0
Deep Eutectic Solvents
0
Monoamine Oxidase Inhibitors
0
Neuroprotective Agents
0
Pyrimidinones
0
Monoamine Oxidase
EC 1.4.3.4
Acetylcholinesterase
EC 3.1.1.7
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
105457Informations de copyright
Copyright © 2021 Elsevier Inc. All rights reserved.