Regioisomeric 3-, 4-and 5-aminomethyl isoxazoles: synthesis and muscarinic activity

…, S Laufer, E Mutschler, J Schweiger, HG Striegel

Index: Dannhardt; Kiefer; Lambrecht; Laufer; Mutschler; Schweiger; Striegel European Journal of Medicinal Chemistry, 1995 , vol. 30, # 11 p. 839 - 850

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Citation Number: 13

Abstract

A series of 3-, 4-and 5-aminomethyl isoxazoles and isoxazoles with one or two additional methyl groups at the heterocycle were synthesized in order to investigate the structural requirements, ie heterocyclic moiety, regiochemistry and length of an aminoalkyl unit, for muscarinic activity. This was assayed on isolated rabbit vas deferens (M1 receptor subtype) and isolated guinea-pig atrium (M2 receptor subtype) and ileum (M3 receptor subtype). ...