FUROXAN类化合物作为NO供体在心血管作用方面的研究  

Study on Furoxan Derivatives as a class of NO donor in Cardiovascular Effect

作　　者：穆莉[1] 华维一[1] 彭司勋[1] 

机构地区：[1]中国药科大学药物化学研究室

出　　处：《药学进展》1997年第1期14-19,共6页Progress in Pharmaceutical Sciences

摘　　要：Ｆｕｒｏｘａｎ即１，２，５－口恶二唑－２－氧化物，具有多种生物活性，近年来对其作为ＮＯ供体的研究较多。本文总结了Ｆｕｒｏｘａｎ类化合物在心血管系统作用方面的研究情况，并结合“ＭｅｄｉｃｉｎａｌＣｈｅｍｉｃａｌＨｙｂｒｉｄｉｚａｔｉｏｎ”方法的应用，列举了已合成的哌唑嗪的Ｆｕｒｏｘａｎ类似物和硝苯地平的Ｆｕｒｏｘａｎ类似物。简介了Ｆｕｒｏｘａｎ释放ＮＯ的机制及有关化合物的构效关系及生物活性。The furoxan (Furazan oxide; 1,2,5 oxadiazole 2 oxide) derivatives possessing wide ranging biological activity have caused much discussion and controversy since its first preparation. The results obtained in the study of the furoxan derivatives as NO donor were reported in the present paper. It was noted that some fused benzofuroxan derivatives, 3,4 disubstituted furoxancarboxamides had the distinct vasodilation effects and 4 methyl 3 (arylsulfonyl)furoxans possessed the most potent inhibiting activity of platelet aggregation among all derivatives concerned. The technique of “medicinal chemical hybridization” or “symbiotic approach” in the design of new drugs for antihypertensive treatment was introduced, and the resulting hybrids, some furoxan analogues of prazosin and nifedipine were described. The mechanism releasing NO from furoxans was also discussed.

关 键 词：NO FUROXAN NO供体 血管扩张作用 

分 类 号：R972.4[医药卫生—药品] R914[医药卫生—药学]