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Novel analogues of ketamine and phencyclidine as NMDA receptor antagonists

2011; Elsevier BV; Volume: 21; Issue: 7 Linguagem: Inglês

10.1016/j.bmcl.2011.02.009

1464-3405

Paola Zarantonello, Ezio Bettini, Alfredo Paio, Chiara Simoncelli, Silvia Terreni, Francesco Cardullo,

Pharmacological Receptor Mechanisms and Effects

The identification of structurally novel analogues of ketamine and phencyclidine (PCP), as NMDA receptor antagonists, with low to moderate potency at GluN2A and GluN2B receptors is discussed. In particular, some examples, such as compounds 6 and 10, shows decreased calculated lipophilicity, when compared to PCP, while retaining moderate activity. Moreover, the germinal aryl amino substituted lactam ring, as exemplified in compounds 7–10 and 11–13, constitutes a novel scaffold with potential application in the design of biologically active compounds.