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

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

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

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被引用次数: 13

摘要

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). ...