Synthesis and central stimulative activities of diaryl(heteraryl) methanesulfinyl acetamide compounds

Aim: To synthesize diaryl(heteraryl) methanesulfinyl acetamide compounds and search for new-type compounds with central stimulative activities. Methods: Target compounds(8a-8t)were synthesized starting from isonicotinic acid via Friedel-Crafts reaction, reduction, substitution, esterification, amination and oxidation. Their central stimulative effects were preliminarily evaluated by the independent activity assay in mice. Results: Twenty target compounds were synthesized and their structures were confirmed by ESI-MS, 1H NMR, IR and elemental analysis. The results of pharmacological test showed that compounds 8a, 8b and 8g enhanced the independent activities of healthy mice (P < 0. 05). Conclusion: Diaryl(heteraryl) methanesulfinyl acetamide compounds possess considerable central stimulative activities.