Synthesis and structure-activity studies of a series of spirooxazolidine-2, 4-diones: 4-oxa-analogs of the muscarinic agonist 2-ethyl-8-methyl-2, 8-diazaspiro [4.5] …

S Tsukamoto, M Ichihara, F Wanibuchi…

Index: Tsukamoto, Shin-ichi; Ichihara, Masato; Wanibuchi, Fumikazu; Usuda, Shinji; Hidaka, Kazuyuki; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 16 p. 2292 - 2299

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Citation Number: 19

Abstract

A series of spirooxazolidine-2, 4-dione derivatives related to the putative MI agonist 2-ethyl- 8-methyl-2, 8-diazaspiro [4.5] decane-1, 3-dione (RS86; 1) were synthesized. The compounds were evaluated as cholinergic agents in in vitro binding assays and in in vivo pharmacological tests including antiamnesic effects using scopolamine-treated mice, hypothermia, and salivation in mice. Four compounds (5a, c, f and 17a) exhibited affinity ...