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Acta Pharmaceutica Sinica ; (12): 372-376, 2013.
Article Dans Chinois | WPRIM | ID: wpr-235657

Résumé

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.


Sujets)
Animaux , Souris , Acétamides , Chimie , Pharmacologie , Comportement animal , Composés benzhydryliques , Chimie , Pharmacologie , Dérivés du biphényle , Chimie , Pharmacologie , Méthane , Chimie , Pharmacologie , Souris de lignée ICR , Répartition aléatoire , Relation structure-activité , Agents promoteurs de l'éveil , Chimie , Pharmacologie
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