Synthesis and Biological Evaluation of Nipecotic Acid and Guvacine Derived 1,3-Disubstituted Allenes as Inhibitors of Murine GABA Transporter mGAT1.
Alkenes
/ chemical synthesis
Animals
Dose-Response Relationship, Drug
Enzyme Inhibitors
/ chemical synthesis
HEK293 Cells
Humans
Mice
Molecular Structure
N-Acetylglucosaminyltransferases
/ antagonists & inhibitors
Nicotinic Acids
/ chemical synthesis
Nipecotic Acids
/ chemical synthesis
Structure-Activity Relationship
GABA uptake inhibitors
allenyl spacer
guvacine
mGAT1
nipecotic acid
Journal
ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013
Informations de publication
Date de publication:
18 06 2019
18 06 2019
Historique:
received:
15
03
2019
pubmed:
9
4
2019
medline:
18
4
2020
entrez:
9
4
2019
Statut:
ppublish
Résumé
A new class of nipecotic acid and guvacine derivatives has been synthesized and characterized for their inhibitory potency at mGAT1-4 and binding affinity for mGAT1. Compounds of the described class are defined by a four-carbon-atom allenyl spacer connecting the nitrogen atom of the nipecotic acid or guvacine head with an aromatic residue. Among the compounds investigated, the mixture of nipecotic acid derivatives rac-{(R
Identifiants
pubmed: 30957949
doi: 10.1002/cmdc.201900170
doi:
Substances chimiques
Alkenes
0
Enzyme Inhibitors
0
Nicotinic Acids
0
Nipecotic Acids
0
nipecotic acid
1U1QTN40SY
guvacine
41538P325K
MGAT1 protein, mouse
EC 2.4.1.-
N-Acetylglucosaminyltransferases
EC 2.4.1.-
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
1135-1151Informations de copyright
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.