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Synthesis and Muscarinic Activity of Isoxazole-substituted 1,2,5,6-Tetrahydropyridines

✍ Scribed by Gerd Dannhardt; Johannes Schweiger; Günter Lambrecht; Ernst Mutschler

Publisher: John Wiley and Sons
Year: 1994
Tongue: English
Weight: 142 KB
Volume: 327
Category: Article
ISSN: 0365-6233
DOI: 10.1002/ardp.19943271115

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✦ Synopsis

Arecoline and other arecaidine esters are semirigid derivatives of the reverse carboxy-analogue of acetylcholine with high muscarinic potencies and intrinsic activities'). Among the arecaidine esters the propargyl derivative 1 is more potent than arecoline and even acetylcholine'). Since the bioisosterism of the isoxazole3) or the oxime ether moiety 24) and the ester group was shown recently, isoxazole substituted tetrahydropyridines were part of our interest.

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