Journal of Medicinal Chemistry p. 761 - 769 (1985)
Update date:2022-08-02
Topics:
Strupczewski, Joseph T.
Allen, Richard C.
Gardner, Beth Ann
Schmid, Blaine L.
Stache, Ulrich
et al.
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 <3H>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-<1-<3-(1,3-dihydro-2-oxo-2H-benzimidazol-1-yl)propyl>-4-piperidinyl>-1,2-benzisoxazole (11b).
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