摘要
磷酸二酯酶5(PDE5)属超家族酶,催化第二信使c GMP转化为GMP。磷酸二酯酶5抑制剂主要用于治疗勃起功能障碍,目前已有多种药物(西地那非、伐地那非等)上市,此外,PDE5抑制剂亦可用于治疗高血压、冠心病和前列腺增生等疾病。本文重点介绍已上市、处于临床试验阶段以及文献报道的PDE5抑制剂,并对其活性及构效关系进行综述。
Phosphodiesterase 5 （PDE5） belongs to the superfamily of enzymes, and can catalyze the second messenger cGMP into GMP. Phosphodiesterase 5 inhibitors were used for the treatment of erectile dysfunction. There are a variety of drugs listed, such as sildenafil, vardenafil and so on. Moreover, PDE5 inhibitors may also be useful in the treatment of hypertension, coronary heart disease and prostate hyperplasia and other diseases. This paper focuses on the PDE5 inhibitors that have listed or in clinical trials and reported in the literature, and reviews its activity and structure-activity relationships.
作者
王林啸
肖玥玥
段永丽
唐启东
WANG Lin-xiao XIAO Yue-yue DUAN Yong-li TANG Qi-dong(School of Pharmacy, Jiangxi Science ＆ Technology Normal University, Nanchang 330013, China)
出处
《中国药物化学杂志》
CAS
CSCD
2017年第5期400-407,共8页
Chinese Journal of Medicinal Chemistry
基金
国家自然科学基金项目(81660572)
