63564-19-2Relevant articles and documents
(E)-(Arylmethyleneaminoxy)acetamides as analogues of neuroleptic benzamides: Synthesis and D2-dopaminergic binding affinity
Macchia,Manera,Martinelli,Orlandini,Romagnoli,Rossello,Chellini
, p. 719 - 724 (2007/10/03)
Some type B (E)-(arylmethyleneaminoxy)acetamides were synthesised as analogues 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 verify whether conformational analogies could exist between type A and type B compounds. Type B compounds were tested for their D2-dopaminergic binding affinity which represents a valid indication of their potential neuroleptic and antipsychotic properties. Biological results indicate that the MAOMM is not able to substitute the aromatic group effectively in the field of neuroleptic benzamides. The results are discussed in the light of the structural analogies and the differences between the MAOMM and the aryl.
Oxime ether derivatives, a new class of nonsteroidal antiinflammatory compounds
Van Dijk,Zwagemakers
, p. 1199 - 1206 (2007/10/07)
A series of new 2-hydroxyethyl and carboxyalkyl ethers of aromatic oximes was found to possess pronounced antiinflammatory activity in the carrageenan-induced edema test in the rat. The activity was limited mainly to derivatives of p-haloacetophenone oxime and of p-halobenzaldehyde oxime. Nevertheless the hydroxyethyl and carboxyalkyl groups may be converted into many derivatives with maintenance of activity. Some structure-activity relationships are in contrast to those of the well-known antiinflammatory arylacetic acids. The activity is limited to the E stereoisomers. The hydrochloride of 2-(dimethylamino)ethyl (E)-[[(p-chloro-α- methylbenzylidene)-amino]oxy]acetate (36, INN name Cloximate) was cosen for clinical evaluation. The first results agree with the pharmacological prospects.
