1-(1,4-苯并二噁烷-2-羰基)-4-取代芳氧烷基哌嗪类α_1受体拮抗剂的合成及其生物活性  

Synthesis and biological activity of 1-(1,4-benzodioxan-2-yl-carbonyl)-4-aryloxy-alkyl-piperazine as α_1-adrenoceptor antagonists

作　　者：李嘉宾[1] 夏霖[1] 王涛[2] 

机构地区：[1]中国药科大学药物化学教研室,江苏南京210009 [2]中国药科大学新中新药研究开发中心,江苏南京210038

出　　处：《中国药物化学杂志》2006年第6期336-341,共6页Chinese Journal of Medicinal Chemistry

基　　金：国家高技术研究发展计划项目(2002AA2Z3118)

摘　　要：目的寻找新的1,4-苯并二烷类α1受体拮抗剂。方法选用1,4-苯并二烷为母核,以儿茶酚和取代苯酚为原料,分别经关环、水解、成酰胺、取代、成盐等反应合成目标化合物,并测定该类化合物α1受体拮抗活性。结果与结论设计合成了13个新化合物,结构经ESI-MS、1H-NMR、IR及HR-MS确证。初步药理活性实验表明,其中8个目标化合物的pA2值大于6.00,具有良好的α1受体拮抗活性,有进一步研究的价值。Aim To find new α1-adrenoceptor antagonists bearing 1, 4-benzodioxane moiety. Methods The target compounds were synthesized from catechol via ring-closing, hydrolysis, amidation, substitution and salt formation. Preliminary biological activities were evaluated. Result and conclusion Thirteen new target compounds were synthesized and their structures were confirmed by ESI-MS, IR, ^1H-NMR, and HR-MS. Biological assay showed the pA2 values of eight target compounds were greater than 6.00. Preliminary bioassay suggested that most of the target compounds showed potent blocking activity to α1-AR and 1-（1,4- benzodioxan-2-yl-carbonyl）-4-aryl-oxyalkylpiperazine should be a kind of valuable α1-adrenoceptor antagonists to be investigated.

关 键 词：药物化学 化合物制备 化学合成 1 4-苯并二噁烷 α1受体拈抗剂 良性前列腺增生 

分 类 号：R914[医药卫生—药物化学]