Volume 27, Issue 18
Isocyclic Compounds
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ChemInform Abstract: (E)-(Arylmethyleneaminoxy)acetamides as Analogues of Neuroleptic Benzamides: Synthesis and D2-Dopaminergic Binding Affinity.

M. MACCHIA

M. MACCHIA

Dip. Sci. Farm., Univ. Pisa, I-56126 Pisa, Italy

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C. MANERA

C. MANERA

Dip. Sci. Farm., Univ. Pisa, I-56126 Pisa, Italy

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A. MARTINELLI

A. MARTINELLI

Dip. Sci. Farm., Univ. Pisa, I-56126 Pisa, Italy

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E. ORLANDINI

E. ORLANDINI

Dip. Sci. Farm., Univ. Pisa, I-56126 Pisa, Italy

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F. ROMAGNOLI

F. ROMAGNOLI

Dip. Sci. Farm., Univ. Pisa, I-56126 Pisa, Italy

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A. ROSSELLO

A. ROSSELLO

Dip. Sci. Farm., Univ. Pisa, I-56126 Pisa, Italy

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G. CHIELLINI

G. CHIELLINI

Dip. Sci. Farm., Univ. Pisa, I-56126 Pisa, Italy

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First published: April 30, 1996

Abstract

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ChemInform Abstract

Analogues of the neuroleptic benzamide metoclopramide and (S)- remoxipride, in which the aromatic group is substituted by a ( methyleneaminooxy)methyl moiety (cf. (V) and (VII), resp.), are synthesized and evaluated for their D2-dopaminergic binding affinity. Biological studies indicate that the (methyleneaminooxy)methyl moiety cannot be considered as a bioisoster of the aryl in neuroleptic benzamides.

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