Bioorganic and Medicinal Chemistry Letters (2019)
Update date:2022-07-31
Topics:
Arita, Tsuyoshi
Asano, Masayoshi
Kubota, Kazufumi
Domon, Yuki
Machinaga, Nobuo
Shimada, Kousei
We synthesized derivatives of a natural alkaloid, conolidine, and evaluated these derivatives in the acetic acid-induced writhing test and formalin test in ddY mice after oral administration. As a result, we identified (5S)-6-methyl-1,3,4,5,6,8-hexahydro-7H-2,5-methano[1,5]diazonino[7,8-b]indol-7-one sulfate salt, 15a (DS54360155), with a unique and original bicyclic skeleton, as an analgesic more potent than conolidine. Moreover, 15a did not exhibit mu-opioid receptor agonist activity.
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