84162-83-4Relevant academic research and scientific papers
Synthesis and Neuroleptic Activity of 3-(1-Substituted-4-piperidinyl)-1,2-benzisoxazoles
Strupczewski, Joseph T.,Allen, Richard C.,Gardner, Beth Ann,Schmid, Blaine L.,Stache, Ulrich,et al.
, p. 761 - 769 (2007/10/02)
The synthesis of a series of 3-(1-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 spiroperidol binding.Structure-activity 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 was a 6-fluoro substituent on the benzisoxazole ring.The 1-piperidinyl substituent appeared less significant, although in most cases, the (1,3-dihydro-2-oxo-2H-benzimidazol-1-yl)propyl group imparted maximum potency.The most potent compound in both assays was 6-fluoro-3--4-piperidinyl>-1,2-benzisoxazole (11b).
3-(4-Piperidyl)-1,2-benzisoxales
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, (2008/06/13)
Novel 3-(4-piperidyl)-1,2-benzisoxazoles, intermediates and processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.
