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Grevellin Analogs with Affinity to the N ‐Methyl‐D‐aspartate (Glycine Site) Receptor, a Novel Lead Structure
Author(s) -
Poschenrieder Hermann,
Höfner Georg,
Stachel HansDietrich
Publication year - 2000
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/1521-4184(20007)333:7<211::aid-ardp211>3.0.co;2-9
Subject(s) - chemistry , glycine , stereochemistry , glycine receptor , piperidine , binding site , potency , receptor , biochemistry , in vitro , amino acid
A series of piperidine‐2,3,5‐triones (azagrevellins) has been prepared. A new synthesis has been introduced using the rearrangement of spiroepoxides in the presence of triethyloxonium tetrafluoroborate. The binding affinity toward 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.