[Synthesis of (+/-)-edulinine analogues].
The natural product, edulinine (I), possesses analgesic, anaesthetic and anticonvulsant activities on the central nervous system. In this paper we report that a series of edulinine analogues IV, V were 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.
Qian
L G
LG
Shanghai Institute of Materia Medica, Academia Sinica.
Gu
K J
KJ
Ji
R Y
RY
D000700:Analgesics / Q000138:chemical synthesis*; D015363:Quinolones / Q000138:chemical synthesis*; D013237:Stereoisomerism
D000700:Analgesics; D015363:Quinolones; C060993:edulinine