Azagrevellins, Part I - Grevellin analogs with affinity to the N-methyl-D-aspartate (glycine site) receptor, a novel lead structure

Authors
Poschenrieder, H Hofner, G Stachel, HD
Citation
H. Poschenrieder et al., Azagrevellins, Part I - Grevellin analogs with affinity to the N-methyl-D-aspartate (glycine site) receptor, a novel lead structure, ARCH PHARM, 333(7), 2000, pp. 211-216
Citations number
25
Categorie Soggetti
Pharmacology & Toxicology
Journal title
ARCHIV DER PHARMAZIE
ISSN journal
03656233 → ACNP
Volume
333
Issue
7
Year of publication
2000
Pages
211 - 216
Database
ISI
SICI code
0365-6233(200007)333:7<211:API-GA>2.0.ZU;2-F
Abstract
A series of piperidine-2,3,5-triones (azagrevellins) has been prepared. A n ew synthesis has been introduced using the rearrangement of spiroepoxides i n the presence of triethyloxonium tetrafluoroborate. The binding affinity t oward the N-methyl-D-aspartate (glycine site) receptor has been measured to provide a basis for more detailed structure-activity studies. Azagrevellin 18d showed the highest binding potency.