Synthesis and neuroleptic activity of 3-(1-substituted-4-piperidinyl)-1, 2-benzisoxazoles

JT Strupczewski, RC Allen, BA Gardner…

Index: Strupczewski, Joseph T.; Allen, Richard C.; Gardner, Beth Ann; Schmid, Blaine L.; Stache, Ulrich; et al. Journal of Medicinal Chemistry, 1985 , vol. 28, # 6 p. 761 - 769

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Citation Number: 87

Abstract

The synthesis of a series of 34 l-substituted-4-piperidinyl)-1, 2-benzisoxazoles is described. The neuroleptic activity of the series was evaluated by utilizing the climbing mice assay and inhibition of [3H] spiroperidol binding. Structureactivity relationships were studied by variation of the substituent on the benzisoxazole ring with concomitant variation of four different 1-piperidinyl substituents. Maximum neuroleptic activity was realized when there ...