1-(5-叔丁基-2-苯并噁唑甲基)-4-(2-取代芳氧基乙基)哌嗪的设计、合成及生物活性  

Design,synthesis and biological activities of 1-(5-t-butyl-2-benzoxazolemethyl)-4-aryloxyalkyl-piperazine as α_1 adrenoceptor antagonists

作　　者：李嘉宾[1] 夏霖[1] 江振洲[2] 

机构地区：[1]中国药科大学药物化学教研室,南京210009 [2]中国药科大学新药筛选中心,南京210038

出　　处：《中国药科大学学报》2006年第2期114-118,共5页Journal of China Pharmaceutical University

基　　金：国家高技术研究发展计划("八六三"计划)资助项目(No.2002AA2Z3118)

摘　　要：目的:寻找新的苯并唑类α1受体拮抗剂。方法:结合α1-受体拮抗剂的构效关系研究,以4-叔丁基-2-氨基酚和取代苯酚为原料,分别经缩合、关环、Williamson醚合成、取代、成盐等反应合成目标化合物,测定α1受体拮抗活性。结果:设计合成了12个新的目标化合物,结构经ESI-MS1、H NMRI、R及HRMS确证。初步药理活性实验表明,7个目标物pA2值大于7.00,有良好的1α受体拮抗活性。结论:5-叔丁基苯并唑芳氧烷基哌嗪类化合物是一类新型的具有潜在价值的α1受体拮抗剂。Aim： To find new α1-adrenoceptor antagonists bearing benzoxazole moiety. Methods： Target compounds were synthesized from 4-t-butyl-2-aminophenol v/a condensation, cycle-closing, substitution and salifieafion; preliminary biological activities were also evaluated. ResultS：Twelve of the new target compounds were synthesized and their structures were confirmed by ESI-MS, IR, 1H NMR and HRMS. Biological assay showed pA2 values of seven target compounds were greater than 7.00. Conclusion： 1-（5- t-butyl-2-benzoxazolemethyl）-4-aryloxyalkyl-piperazine is potentially a new candidate for α1 adrenoceptor antagonist.

关 键 词：苯并噁唑 α1-肾上腺素受体拮抗剂 良性前列腺增生 合成 

分 类 号：O626.2[理学—有机化学]