α-苯基取代肉桂酰胺类化合物的合成及其钾通道开放活性  

SYNTHESIS AND VASODILATIVE ACTIVITIES OF α-PHENYLCINNAMIDE

作　　者：牟丽媛[1] 林紫云[1] 朱莉亚[1] 梁晓天[1] 

机构地区：[1]中国医学科学院,中国协和医科大学药物研究所,北京100050

出　　处：《药学学报》2001年第7期502-506,共5页Acta Pharmaceutica Sinica

摘　　要：目的　寻找新的降压药物。方法和结果　以N (4 甲氧基苯甲酰基 ) N′ 肉桂基哌嗪为先导物 ,用混合酸酐法和酰氯法合成了 2 2个α 苯基取代的肉桂酰胺类衍生物 ,这些化合物均为新化合物。用MS和1 HNMR确证了其结构。结论　生物活性筛选结果表明 ,大部分化合物对去甲肾上腺素引起的大鼠主动脉条收缩有较好的抑制作用 ,一些化合物 (3,9,11)对去甲肾上腺素和高钾收缩的抑制作用优于先导物 ,其中化合物AIM To search for compounds having strong vasodilating effect. METHODS AND RESULTS The mixed anhydride and α phenylcinnamyl halide were used. Twenty two α phenylcinnamide derivatives were synthesized. The strutures were elucidated on the basis of MS and 1HNMR . Compounds 1-22 are new compounds. CONCLUSION Vasodilative activity assays were conducted for the target compounds and the results indicated that several compounds (3, 9 and 11) demonstrated superior pharmacological profiles to the lead compound,among which compound 11 was further evaluated and found to be indicative of potential KCO activity. Preliminary SAR of α phenylcinnamides was discussed herein.

关 键 词：α-苯基取代肉桂酰胺 扩血管活性 钾通道开放剂 合成 

分 类 号：R972.4[医药卫生—药品] R914.5[医药卫生—药学]