A series of novel helicid derivatives containing 1,3,4-oxadiazole 3a～3g were successfully synthesized from the intermediates aryl-3-carbonyl (4-β-D-allopyranoside-yl)-benzaldehyde hydrazone derivatives (2a～2g), which prepared starting from helicid. The new compounds were characterized by ¹H NMR, IR and HR-MS spectra. The sedative-hypnotic activities of the target compounds 3a～3g were evaluated by testing the spontaneous locomotor activity in mice. All of the derivatives produced moderate to high activities. In particularly, compound 3c presented the most potent sedative-hypnotic effect in comparison to the other derivatives, and compounds 3a and 3f also showed potent activities.

Key words: helicid, calm activity, 1,3,4-oxadiazole, synthesis, cyclization