Stereochemical properties of quazepam and its affinity for the GABAA receptor.
Bioorg Med Chem Lett
; 110: 129854, 2024 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-38914347
ABSTRACT
C9-methylated quazepam 1 was prepared, and its physicochemical properties were investigated. The atropisomers of 1 were isolated as (a1R, a2S) and (a1S, a2R) isomers. Their absolute configurations were determined based on ECD spectra in comparison with those calculated using the time-dependent density functional theory. Preliminary examination of affinity for the GABAA receptor revealed that the (a1R, a2S) isomer of 1 possessed higher activity than its antipode (a1S, a2R) isomer. The active configuration of C9-methylated quazepam 1 is the same as that of 1,4-benzodiazepin-2-ones.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptores de GABA-A
Limite:
Humans
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article