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(E)-(methyloxyimino)acetamides as analogues of neuroleptic benzamides: synthesis and D2-dopaminergic binding affinity
A Lapucci1, M Macchia, E Orlandini
1Dipartimento di Scienze Farmaceutiche, Università di Pisa, Italy.
Abstract:
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 (CH2ON = CH, E-MOIMM). Type C compounds were tested for their D2-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 D2-dopaminergic receptor, at least one order of magnitude lower than that of metoclopramide and sulpiride.
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