Design, synthesis, and evaluation of polyamine-memantine hybrids as NMDA channel blockers

Publication date: Available online 16 December 2017
Source:Bioorganic & Medicinal Chemistry
Author(s): Takuya Kumamoto, Marie Nakajima, Reina Uga, Naoko Ihayazak, Haruna Kashihara, Kazuaki Katakawa, Tsutomu Ishikawa, Ryotaro Saiki, Kazuhiro Nishimura, Kazuei Igarashi
N-Methyl-D-aspartate (NMDA) receptors have been implicated in learning and memory, and may also play a central role in various conditions leading to neuronal degradation. NMDA receptor antagonists could therefore be of therapeutic benefit for a number of neurological disorders. We have designed hybrid compounds of polyamines and memantine, both of which function as NMDA channel blockers. The triamine derivative with a guanidine moiety showed more potent antagonistic activity than memantine.

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