Synthesis and biological activity of indoline compounds as α_1-AR antagonist

VernacularTitle:吲哚啉类α_1-肾上腺素受体拮抗剂的合成及生物活性
Author: Jiangbo ZHANG ; Guohua CHEN ; Xiaochuan LUO ; Feihua WU
Publication Type:Journal Article
Keywords: silodosin; 1-[( substituted phenoxy) alkyl] piperazine; indoline; α_1-adrenoceptor; benign prostate hyperplasia; synthesis
From: Journal of China Pharmaceutical University 2009;40(3):200-204
CountryChina
Language:Chinese
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.