N-(3,4-二甲氧基苯乙基)-4-取代苯基哌嗪-1-乙酰胺类α_1-受体拮抗剂的合成及其生物活性

Synthesis and Biological Activity Study on N-(3,4-Dimethox yphenylethyl)-4-Subtituted Phenylpiperazine-1-Acetamide Series as α_1-Adrenoceptor Antagonists

目的 :研究 3 ,4 二甲氧基苯乙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、取代和胺解反应合成目的物 ;测定目的物体外α1 受体拮抗活性。结果 :设计、合成了 14个新化合物(WBⅡ 1～ 14 ) ,其结构均经IR、1 HNMR、ESI MS确证。化合物WBⅡ 6、WBⅡ 7、WBⅡ 10和WBⅡ 12对大鼠肛尾肌动脉环有一定的抑制作用 ,抑制率高于 50 %。结论 :初步生物活性测试表明 ,所合成的化合物活性 (pA2 )

AIM: To study the synthesis and anti α 1-a drenoceptor activity of 3,4-dimethoxyphenylethylamino phenylpiperazine compound s METHOD:Cyclization,substitution and amidation reactions were used in t he synthesis of the title compoundsThe inhibition activity of the target compoun ds were tested RESULT: Fourteen new compounds were synthesized Structure of the title compounds were determined by IR, 1HNMR and ESI-MS Compounds WBⅡ-6,WBⅡ-7,WBⅡ-10 and WBⅡ-12 showed the inhibito ry activity(>50%) on rat anococcygeal musclesCONCLUSION:The po tency (pA 2) of the title compounds were lowe r than that of control Prazosin