Isoxazole Derivatives as Centrally Acting Muscle Relaxants. III. : Synthesis and Activity of Conformationally Restricted Analogs(Medeicinal Chemistry,Chemical)

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Conformationally restricted analogs of muscle-relaxant 3-amino-2-methyl-N-(3-phenyl-5-isoxazolyl)propanamides (1) and 5-(3-aminopropylamino)-3-phenylisoxazoles (2) were prepared, and their muscle-relaxant and other pharmacological activities were tested and compared with those of the corresponding acyclic derivatives. 7-(3-Diethylamino-2-methylpropanoyl)-3-phenyl-4,5,6,7-tetrahydroisoxazolo[5,4-b]pyridine (8) exhibited muscle-relaxant and anticonvulsant activities comparable with those of corresponding acyclic derivatives, i.e. 3-diethylamino-2-methyl-N-(3-phenyl-5-isoxazolyl)propanamides (1e-g), but other types of compounds showed decreased activities. The preferred conformation of the present isoxazole derivatives for muscle-relaxant activity is discussed. 7-Benzyl-6-methyl-3-phenyl-4-pyrrolidino-4,5,6,7-tetrahydroisoxazolo[5,4-b]pyridine (3d) showed moderate central nervous system-depressant activity.
公益社団法人日本薬学会の論文
1987-09-25