Modulating physicochemical properties of tetrahydropyridine-2-amine BACE1 inhibitors with electron-withdrawing groups: A systematic study.
Amidines
/ chemistry
Amyloid Precursor Protein Secretases
/ antagonists & inhibitors
Animals
Aspartic Acid Endopeptidases
/ antagonists & inhibitors
Chemistry, Physical
Dogs
Dose-Response Relationship, Drug
Electrons
Enzyme Inhibitors
/ chemical synthesis
Humans
Molecular Structure
Pyrrolidines
/ chemical synthesis
Structure-Activity Relationship
Alzheimer's
Amidine
BACE1
EPSA
logD
pK(a)
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
15 Jan 2022
15 Jan 2022
Historique:
received:
03
09
2021
revised:
20
11
2021
accepted:
26
11
2021
pubmed:
18
12
2021
medline:
27
1
2022
entrez:
17
12
2021
Statut:
ppublish
Résumé
A common challenge for medicinal chemists is to reduce the pK
Identifiants
pubmed: 34920170
pii: S0223-5234(21)00877-1
doi: 10.1016/j.ejmech.2021.114028
pii:
doi:
Substances chimiques
Amidines
0
Enzyme Inhibitors
0
Pyrrolidines
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
Pagination
114028Informations de copyright
Copyright © 2021 Elsevier Masson SAS. 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.