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■ Synthesis of Two Novel Water-soluble Cleft-Type Cyclophanes Effective as N-Methyl-D-aspartate Receptor Antagonist

Takashi Masuko, Yuta Nemoto, Tadashi Kusama, Koichi Metori, Yasuo Kizawa, and Muneharu Miyake*

*College of Pharmacy, Nihon University, 7-7-1 Narashinodai, Funabashi-shi, Chiba 274-8555, Japan

Abstract

Novel cleft-type cyclophanes, 4,4′-bis[N-(5-dimethylaminonaphthalene-sulfonylaminoethyl)-N-(1,4,7,10-tetraazacyclododecane-1-ylacetyl)-2-aminoethoxy]diphenylmethane octahydrochloride (1a, DNCn) and 4,4′-bis[N-(p-toluene-sulfonylaminoethyl)-N-(1,4,7,10-tetraazacyclododecane-1-ylacetyl-2-aminoethoxy]diphenylmethane octahydrochloride (1b, TsDCn) having an effective role as N-methyl-D-aspartate (NMDA) receptor antagonist were synthesized. Neuroprotective effects of cleft-type cyclophanes, DNCn (1a) and TsDCn (1b) against cell damage caused by NMDA were measured in cultured rat hippocampal neurons. DNCn (1a) and TsDCn (1b) reduced the neurotoxicity and acted as open channel blocker for NMDA receptor.