Synthesis and biological activity of indoline compounds as α_1-AR antagonist / 中国药科大学学报

ABSTRACT

Aim: To search for novel α_1-adrenoceptor(α_1-AR) antagonists. Methods: On the basis of hybridization principle with silodosin as the lead compound, twelve 5-[2-[4-[ ( substituted phenoxy) alkyl] piperazin-1-yl] propyl] indoline compounds were designed and synthesized by maintaining indoline while incorporating the 1-[(substituted phenoxy) alkyl] piperazine group. Results: The structures of synthesized target compounds were confirmed by the elemental analysis, IR, ESI-MS and ~1H NMR. Preliminary pharmacological test showed that pA_2 values of six target compounds were greater than 7. 50, which suggested that the compounds possessed considerable α_1-AR antagonic activity. Conclusion: 5-[2-[4-[ ( substituted phenoxy) alkyl] piperazin-1-yl] propyl] indoline compounds is potentially a new candidate for α_1-AR antagonist.