One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues.
Alzheimer’s disease
BACE-1 inhibitors
Biginelli reaction
dihydropyrimidinones
β-secretase
Journal
Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009
Informations de publication
Date de publication:
10 Sep 2020
10 Sep 2020
Historique:
received:
30
07
2020
revised:
31
08
2020
accepted:
02
09
2020
entrez:
15
9
2020
pubmed:
16
9
2020
medline:
16
3
2021
Statut:
epublish
Résumé
A library of dihydropyrimidinones was synthesized via a "one-pot" three component Biginelli reaction using different aldehydes in combination with β-dicarbonyl compounds and urea. Selected 2-thiooxo and 2-imino analogs were also obtained with the Biginelli reaction from thiourea and guanidine hydrochloride, respectively. The products were screened in vitro for their β-secretase inhibitory activity. The majority of the compounds resulted to be active, with IC
Identifiants
pubmed: 32927879
pii: molecules25184152
doi: 10.3390/molecules25184152
pmc: PMC7571164
pii:
doi:
Substances chimiques
Pyrimidinones
0
Amyloid Precursor Protein Secretases
EC 3.4.-
Aspartic Acid Endopeptidases
EC 3.4.23.-
BACE1 protein, human
EC 3.4.23.46
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Università degli Studi di Trieste
ID : FRA 2016
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