Indoline analogs of idazoxan: potent .alpha.2-antagonists and .alpha.1-agonists

摘要: The synthesis and alpha-adrenergic activity of a series substituted 2-imidazolinylindolines are described. Substitution in the indoline ring generated compounds with spectrum adrenoceptor antagonist/agonist profiles that proved sensitive to both nature position substituent. Many derivatives possess greater presynaptic antagonist potency than corresponding benzodioxan 1, dihydrobenzofuran 2, indan 3 analogues; however, this alpha 2-antagonism is often accompanied by 1-agonist activity. It was not possible separate 2-antagonist from properties series. Compounds most interest be N-ethyl 6, 5-chloro-N-methyl 18, 5-chloro-N-ethyl 23 derivatives, all being potent 2-antagonists 1-agonists. at 4- 7-position generally gave nonselective agonist properties.