Isoxazole derivatives as centrally acting muscle relaxants. III. Synthesis and activity of conformationally restricted analogs.

…, H YAMANAKA, M MIZUGAKI, T SAKAMOTO…

Index: Tatee; Narita; Kurashige; Ito; Miyazaki; Yamanaka; Mizugaki; Sakamoto; Fukuda Chemical and Pharmaceutical Bulletin, 1986 , vol. 34, # 4 p. 1643 - 1655

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Citation Number: 11

Abstract

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 ...