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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

NR2B Selective NMDA Antagonists: The Evolution of the Ifenprodil-Type Pharmacophore

Author(s): Istvan Borza and Gyorgy Domany

Volume 6, Issue 7, 2006

Page: [687 - 695] Pages: 9

DOI: 10.2174/156802606776894456

Price: $65

Abstract

The quest for NR2B subtype selective NMDA antagonists started almost twenty years ago. The structure of ifenprodil, the prototype of this group of compounds, inspired many medicinal chemists in several research units. Different approaches led to the identification of the pharmacophore and several distinct classes of compounds containing this pharmacophore. From these studies a few drug candidates emerged and clinical trials proved the viability of the concept. This article attempted to follow the evolution from ifenprodil, a multiple ligand, to selective NR2B antagonists.

Keywords: Ifenprodil, NR2B subunit, pharmacophore, side activities, piperidines


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