Synthesis and biological evaluation of 1-(1, 2-benzisothiazol-3-yl)-and (1, 2-benzisoxazol-3-yl) piperazine derivatives as potential antipsychotic agents

JP Yevich, JS New, DW Smith, WG Lobeck…

Index: Yevich, Joseph P.; New, James S.; Smith, David W.; Lobeck, Walter G.; Catt, John D.; et al. Journal of Medicinal Chemistry, 1986 , vol. 29, # 3 p. 359 - 369

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Citation Number: 122

Abstract

Members of the series of title compounds were tested for potential antipsychotic activity in relevant receptor binding assays and behavioral screens. Structure-activity relationships within the series are discussed. Compound 24 (BMY 13859-l), a (1, 2-benzisothiazol-3-yl) piperazine derivative, was selected for further study because of its potent and selective profile in primary CNS tests. It was active in the Sidman avoidance paradigm and blocked ...