摘要
在寻找先导化合物的过程中,苯并硫氮杂类化合物占有非常重要的位置。按照结构类型,苯并硫氮杂类主要包括1,3-、1,4-、4,1-和1,5-苯并硫氮杂四大类。它们可以作用于许多不同家族的靶点,显示出了广泛的生物学活性。在苯并硫氮杂类化合物中,1,5-苯并硫氮杂类化合物的生物学活性最为广泛,可以作为钙离子通道拮抗剂、某些蛋白激酶的抑制剂、一些G蛋白偶联受体的拮抗剂以及缓激肽激动剂等。作者对苯并硫氮杂类化合物的研究进展进行了综述。
Benzothiazepine derivatives are of great importance in the discovery of lead compounds. Benzothiazepine can be devided into four types according to structure, i. e. 1, 3-, 1, 4-, 4, 1- and 1, 5-benzothiazepine. They can act on different families of targets and show wide range of biological activities. Among all the benzothiazepine derivatives, 1,5-benzothiazepine derivatives was the most important because of its wide biological activities. They can be used as calcium channel blockers, protease inhibitors, antagonists of several G-protein-coupled receptors and bradykinin agonists. In this article, the biological activities and synthetic methods are reviewed.
出处
《中国药物化学杂志》
CAS
CSCD
2007年第2期122-128,共7页
Chinese Journal of Medicinal Chemistry
