Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists

…, JT Drummond, G Johnson, T Malone…

Index: Bigge; Drummond; Johnson; Malone; Probert Jr.; Marcoux; Coughenour; Brahce Journal of Medicinal Chemistry, 1989 , vol. 32, # 7 p. 1580 - 1590

Full Text: HTML

Citation Number: 51

Abstract

To investigate the preferred spatial relationship of the distal phosphonic acid to the a-amino acid group of the established competitive N-methyl-D-aspartic acid (NMDA) antagonists APH (1) and APV (2), we have prepared a series of ortho-, meta-, and para-substituted (phosphonoalky1) phenylglycine and-phenylalanine derivatives. With use of a [3H] CPP receptor binding assay, significant binding activity was observed to be critically dependent ...