Synthesis and biological evaluation of novel diphenyl methane sulfinyl and diphenylthio-acetamide derivatives.
- Author:
Xiong ZHU
1
;
Yan TANG
;
Cong GAO
;
Liu-Quan ZHANG
;
Wen-Long HUANG
Author Information
1. Medicinal and Chemical Institute, China Pharmaceutical University, Nanjing 210009, China.
- Publication Type:Journal Article
- MeSH:
Acetamides;
chemical synthesis;
chemistry;
pharmacology;
Animals;
Behavior, Animal;
drug effects;
Benzhydryl Compounds;
chemistry;
pharmacology;
Biphenyl Compounds;
chemical synthesis;
chemistry;
pharmacology;
Methane;
chemical synthesis;
chemistry;
pharmacology;
Mice;
Mice, Inbred ICR;
Random Allocation;
Structure-Activity Relationship;
Wakefulness-Promoting Agents;
chemical synthesis;
chemistry;
pharmacology
- From:
Acta Pharmaceutica Sinica
2013;48(3):372-376
- CountryChina
- Language:Chinese
-
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.
