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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。
OBJECTIVE: To find new benzoxazole α1 receptor antagonists. Methods: The structure-activity relationship of α1-receptor antagonist was studied. 4-tert-Butyl-2-aminophenol and substituted phenol were used as starting materials to synthesize, The target compound was tested for α1 receptor antagonistic activity. RESULTS: Twelve new target compounds were designed and synthesized. Their structures were confirmed by ESI-MS1, H NMR, R and HRMS. Preliminary pharmacological activity experiments showed that 7 target pA2 value of greater than 7.00, a good antagonist of 1α receptor. CONCLUSION: 5-tert-Butylbenzoxazole aryloxyalkylpiperazines are a new class of potential α1 receptor antagonists.