Melloni P, Banzatti C, Heidempergher F, Marazzi G, Ricciardi S, Vaghi F, Varasi M
Farmitalia Carlo Erba Research & Development, Erbamont Group, Milano, Italy.
Farmaco. 1991 Sep;46(9):1011-21.
The synthesis of new 2-imidazol(in)yl-alkyl derivatives of 2,3,3a,4-tetrahydro-1H-imidazo[5,1-c][1,4]benzoxazin-1-one is reported. Some compounds of the series have shown high affinity for alpha 2 receptors, high alpha 2/alpha 1 selectivity and alpha 2 antagonism in vitro (vas deferens). Owing to their selective alpha 2-antagonism associated to a novel structure, compounds 8 and 20 have been selected for further biological investigation as potential antidepressants.
报道了2,3,3a,4-四氢-1H-咪唑并[5,1-c][1,4]苯并恶嗪-1-酮的新型2-咪唑（啉）基-烷基衍生物的合成。该系列中的一些化合物在体外（输精管）对α2受体表现出高亲和力、高α2/α1选择性和α2拮抗作用。由于化合物8和20具有与新结构相关的选择性α2拮抗作用，已被选作潜在抗抑郁药进行进一步的生物学研究。
