Synthesis and biological activity of indoline compounds as α₁-AR antagonist

Aim ：To search for novel α₁-adrenoceptor(α₁-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 pA₂ values of six target compounds were greater than 7.50，which suggested that the compounds possessed considerable α₁-AR antagonic activity. Conclusion ：5-［2-［4-［(substituted phenoxy)alkyl］piperazin-1-yl］propyl］indoline compounds is potentially a new candidate for α₁-AR antagonist.