摘要
目的 :研究 5 甲氧基色胺苯基哌嗪衍生物的合成及其α1 受体拮抗活性。方法 :由取代苯胺通过环合、取代和胺解等反应合成目的物 ;测定目的物体外α1 受体拮抗活性。结果 :合成了 14个新化合物 ,其结构经IR ,1HNMR和ESI MS质谱确证 ;化合物WBⅠ 2、WBⅠ 3、WBⅠ 4、WBⅠ 8、WBⅠ 9和WBⅠ 14对大鼠肛尾肌动脉环有一定的抑制作用 (抑制率大于 5 0 % )。结论 :初步生物活性测试表明 ,所合成的化合物活性 (pA2 )低于阳性对照药哌唑嗪。
AIM: To study the synthesis and anti-α_ 1 -adrenoceptor activity of 5-methoxytryptamine phenylpiperazine compounds. METHOD: Cyclization,substitution and amidation reactions were used in the synthesis of the title compounds.The inhibition activity of the target compounds were tested. RESULT: Fourteen new compounds were synthesized. Structure of the title compounds were determined by IR, 1 HNMR and ESI-MS. Compounds WBⅠ-2,WBⅠ-3,WBⅠ-4,WBⅠ-8,WBⅠ-9 and WBⅠ-14 showed inhibition activity. CONCLUSION: The potency (pA_ 2 ) of the title compounds was lower than those of control Prazosin.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2003年第5期391-395,共5页
Journal of China Pharmaceutical University
基金
国家"8 63"项目基金资助 (编号 2 0 0 2AA2Z3 118)~~
关键词
苯基哌嗪
5-甲氧基色胺
α1-受体拮抗剂
合成
活性
Phenylpiperazine
5-Methoxytryptamine
α_1-Adrenoceptor antagonists
Synthesis
Activity
