Abstract
Herein, we report novel orexin antagonists with a spiro-type piperidine skeleton designed and synthesized via removal of the unnecessary sites of orexin 1 receptor (OX1R) antagonists with a morphinan skeleton for binding to OX1R. In addition, while decahydroisoquinoline compounds with an A-ring did not show antagonistic activity for OX1R, spiro-type piperidine compounds with a dihydroindene structure showed antagonistic activities. This suggests that the lipophilic site corresponding to the A-ring of the morphinan skeleton is important for determining the antagonistic activity toward OX1R.
Original language | English (US) |
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Journal | Heterocycles |
Volume | 103 |
Issue number | 2 |
DOIs | |
State | Published - 2021 |
Externally published | Yes |
ASJC Scopus subject areas
- Analytical Chemistry
- Pharmacology
- Organic Chemistry