芳基磺胺类内皮素受体拮抗剂的研究与开发  

Development of Arylsulfonamide Endothelin Receptor Antagonists

作　　者：陈志龙[1] 陈静蓉[1] 王建国[1] 张黎明[1] 孙结[1] 

机构地区：[1]第二军医大学海军医学系毒物药物研究室,上海200433

出　　处：《药学进展》2001年第6期321-326,共6页Progress in Pharmaceutical Sciences

摘　　要：内皮素ET 1是目前已知的活性最强的缩血管因子 ,与蛛网膜下腔出血、颅内动脉瘤破裂、脑中风、高血压、肾衰、充血性心衰、哮喘等疾病的发生、发展密切相关。芳基磺胺是一类重要的非肽类内皮素受体拮抗剂 ,综述该类拮抗剂的研究与开发 ,并介绍其构效关系。Endothelins (ETs) are a family of potent vasoactive peptides associated with the pathophysiology of certain cardiovascular and renal diseases, of which ET-1 is known as the most potent mammalian vasoconstrictor peptide. The development of potent, subtype selective and orally active endothelin antagonists was of great interest for several major clinical indications including hypertension, renal failure, asthma and circulatory conditions. The advances in arylsulfonamide endothelin receptor antagonists were reviewed. Their structures and structure-activity relationships were briefly introduced,too.

关 键 词：内皮素 内皮素受体拮抗剂 芳基磺胺 磺胺类药物 

分 类 号：R944[医药卫生—药剂学]