Syntheses and Pharmacological Evaluations of Novel N-substituted Bicyclo-heptan-2-amines at NMDA Receptors

Several novel norcamphor (bicycloheptane) based compounds were designed and synthesized as noncompetitive NMDA receptor antagonists at the Phencyclidine (PCP) binding sites. The heterocyclic ring was also varied to examine piperidine, pyrrolidine and morpholine groups. We examined pharmacological ac...

Full description

Saved in:
Bibliographic Details
Published in:Chemical biology & drug design 2011-05, Vol.78 (1), p.25-32
Main Authors: Ates-Alagoz, Zeynep, Sun, Shengguo, Wallach, Jason, Adejare, Adeboye
Format: Article
Language:English
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Several novel norcamphor (bicycloheptane) based compounds were designed and synthesized as noncompetitive NMDA receptor antagonists at the Phencyclidine (PCP) binding sites. The heterocyclic ring was also varied to examine piperidine, pyrrolidine and morpholine groups. We examined pharmacological activities of these compounds in vitro (binding studies) and in vivo (MES test). Pharmacological evaluations revealed one of the compounds, 5a, to be a good lead, exhibiting moderate binding at NMDA receptors (IC 50 = 7.86 μM; K i = 5.28 μM), MES neuroprotection activity at 100 mg/kg and acceptable toxicity profile.
ISSN:1747-0277
1747-0285
DOI:10.1111/j.1747-0285.2011.01124.x