Abstract: The natural product, edulinine (Ⅰ), possesses analgesic, anaesthetic and anticonvulsant activities on the central nervous system. In this paper we report that a series ofedulinine analogues Ⅳ, Ⅴwere synthesized and screened in mice according to methods of Topliss and Austel quantitative drug design. In preliminary pharmacological tests a number of synthesized compounds showed central depressant activities stronger than edulinine.