(E)-(ARYLMETHYLENEAMINOXY)ACETAMIDES AS ANALOGS OF NEUROLEPTIC BENZAMIDES - SYNTHESIS AND D-2-DOPAMINERGIC BINDING-AFFINITY

Citation
M. Macchia et al., (E)-(ARYLMETHYLENEAMINOXY)ACETAMIDES AS ANALOGS OF NEUROLEPTIC BENZAMIDES - SYNTHESIS AND D-2-DOPAMINERGIC BINDING-AFFINITY, Il Farmaco, 50(10), 1995, pp. 719-724
Citations number
18
Categorie Soggetti
Pharmacology & Pharmacy
Journal title
ISSN journal
0014827X
Volume
50
Issue
10
Year of publication
1995
Pages
719 - 724
Database
ISI
SICI code
0014-827X(1995)50:10<719:(AAONB>2.0.ZU;2-X
Abstract
Some type B (E)-(arylmethyleneaminoxy)acetamides were synthesised as a nalogues of type A neuroleptic and antipsychotic benzamides, in which the aromatic group is substituted by a (methyleneaminoxy)methyl moiety (C = NOCH2, MAOMM). Theoretical studies were performed in order to ve rify whether conformational analogies could exist between type A and t ype B compounds. Type B compounds were tested for their D-2-dopaminerg ic binding affinity which represents a valid indication of their poten tial neuroleptic and antipsychotic properties. Biological results indi cate that the MAOMM is not able to substitute the aromatic group effec tively in the field of neuroleptic benzamides. The results are discuss ed in the light of the structural analogies and the differences betwee n the MAOMM and the aryl.