Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines as potential central nervous system agents. 2. Compounds containing a heteroatom attached to nitrogen

Abstract
The synthesis and antitetrabenazine activity of a series of N-heteroatom derivatives of 3-phenylspiro[isobenzofuran-1,4''-piperidines] were reported. Optimal antitetrabenazine activity was associated with compounds containing a sterically unhindered, basic nitrogen. Certain hydroxylamines possessed the most significant activity with ED50s of 1.4, 3.5, 4.7, and 4.0 [in mice].

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