J. Med. Chem

Drug Design, in Vitro Pharmacology, and Structure− Activity Relationships of 3-Acylamino-2-aminopropionic Acid Derivatives, a Novel Class of Partial Agonists at the …

S Urwyler, P Floersheim, BL Roy, M Koller

Index: Urwyler, Stephan; Floersheim, Philipp; Roy, Bernard L.; Koller, Manuel Journal of Medicinal Chemistry, 2009 , vol. 52, # 16 p. 5093 - 5107

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Citation Number: 11

Abstract

Retaining agonistic activity at the glycine coagonist site of the NMDA receptor in molecules derived from glycine or D-serine has proven to be difficult because in the vicinity of the R- amino acid group little substitution is tolerated. We have solved this problem by replacing the hydroxy group of D-serine with an amido group, thus keeping the hydrogen donor function and allowing for further substitution and exploration of the adjacent space. ...