Synthesis and biological evaluation of novel diphenyl methane sulfinyl and diphenylthio-acetamide derivatives / 药学学报
Acta Pharmaceutica Sinica
;
(12): 372-376, 2013.
Article
Dans Chinois
| WPRIM
| ID: wpr-235657
ABSTRACT
According to the structure-activity relationships (SARs) of modafinil, a therapeutic drug of hypnolepsy, we designed and synthesized two series of compounds 2-[(diphenylmethane)sulfinyl] acetamides and 2-[(diphenylmethyl)thio] acetamides, and measured their biological activities. The target compounds (6a-6o) were synthesized beginning with diphenyl carbinol by substitution, oxidation, acylation and so on. Their structures were confirmed by ESI-MS, 1H NMR and elemental analysis. The central stimulatory effects of the target compounds were determined by the independent activity assay on mice. Compounds 6c, 6f and 6n have considerable activities, while the central stimulative effect of 6h is slightly better than the positive control modafinil.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Pharmacologie
/
Relation structure-activité
/
Comportement animal
/
Composés benzhydryliques
/
Dérivés du biphényle
/
Répartition aléatoire
/
Chimie
/
Agents promoteurs de l'éveil
/
Acétamides
/
Méthane
Limites du sujet:
Animaux
langue:
Chinois
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2013
Type:
Article
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