Some 2-[(methyleneamino)oxy]-N-(guanidino)ethaneimines were synthesized as analogs of guanabenz-type benzylideneaminoguanidine α2-agonists in which the aryl portion (Ar) is substituted by the [(methyleneamino)oxy]methyl moiety (MAOMM). The α2-adrenergic activity of the synthesized MAOMM derivs. was evaluated by functional tests on guinea-pig ileum. The MAOMM-derivs. exhibited an α2-adrenergic stimulating activity fairly similar to that of the benzylideneaminoguanidine ref. drug guanabenz, thus supporting the hypothesis of the existence of a bioisostere-like relationship between the MAOMM and the Ar in the class of guanabenz-type α2-adrenergic agonists.
|Autori:||A. BALSAMO; D. GENTILI; M. MACCHIA; E. MARTINOTTI; R. SCATIZZI; ROSSELLO A|
|Titolo:||Synthesis and α2-adrenergic activity of 2-[(methyleneamino)oxy]-N-(guanidino)ethaneimines. A bioisosteric replacement of the aryl of guanabenz-type benzylideneaminoguanidine α2-agonists with the [(methyleneamino)oxy]methyl moiety (MAOMM)|
|Anno del prodotto:||1996|
|Digital Object Identifier (DOI):||10.1016/0223-5234(96)85880-6|
|Appare nelle tipologie:||1.1 Articolo in rivista|