(E) - (methyloxyimino) acetamides as analogues of neuroleptic benzamides: synthesis and D2-dopaminergic binding affinity

Lapucci, A.; Macchia, M.; Orlandini, E.; Romagnoli, F.; Rossello, A.; Chiellini, G.; Cozzini, P.; Domiano, P.

Farmaco 51(1): 33-39

1996


ISSN/ISBN: 0014-827X
PMID: 8721759
Document Number: 455811
Some type C (E)-(methyloxyimino)acetamides were synthesised as analogues of type A neuroleptic and antipsychotic benzamides, in which the aromatic group is substituted by a methyloxyiminomethyl moiety with the E configuration (CH-2ON = CH, E-MOIMM). Type C compounds were tested for their D-2-dopaminergic binding affinity in order to obtain an indication of their potential neuroleptic and antipsychotic properties. Biological results showed that only a few aryl-substituted E-MOIM derivatives possess a certain affinity for the D-2-dopaminergic receptor, at least one order of magnitude lower than that of metoclopramide and sulpiride.

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