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Syntheses of Biphenyl Analogues of AP7, a New Class of Competitive N-Methyl-D-aspartate (NMDA) Receptor Antagonists

✍ Scribed by Werner Müller; Peter Kipfer; David A. Lowe; Stephan Urwyler

Publisher
John Wiley and Sons
Year
1995
Tongue
German
Weight
676 KB
Volume
78
Category
Article
ISSN
0018-019X

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✦ Synopsis

Abstract

Syntheses of a series of enantiomerically pure, substituted analogues 7b–t of SDZ EAB 515 (7a) were described (Schemes 1 and 2). Affinites for the NMDA receptor were measured ([^3^H]CGP‐39653 binding assay) and competitive NMDA antagonistic potencies determined in a functional test (rat neocortical slice preparation). Structure‐activity relationships show that attachment of an OH group at position 4 of the chain‐inserted benzene ring of the biphenyl moiety and/or expansion of the angle between the planes of the two benzene rings by ortho‐substituents increase in vitro activities into the low nanomolar range.

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