新型源自氰肽的类胰蛋白酶丝氨酸蛋白酶低分子量抑制剂。

New cyanopeptide-derived low molecular weight inhibitors of trypsin-like serine proteases.

作者信息

Radau Gregor, Schermuly Sonja, Fritsche Alexandra

机构信息

Institute of Pharmacy, Ernst-Moritz-Arndt-University Greifswald, Pharmaceutical/Medicinal Chemistry, Greifswald, Germany.

出版信息

Arch Pharm (Weinheim). 2003 Aug;336(6-7):300-9. doi: 10.1002/ardp.200300765.

DOI:10.1002/ardp.200300765

PMID:12953218

Abstract

This paper deals with the design, syntheses, and inhibition tests of new low molecular weight thrombin inhibitors utilizing cyanopeptides, the secondary metabolites of cyanobacteria with interesting biological activities, as new lead structures. Starting with aeruginosin 98-B (1) as a lead structure, we have developed and synthesised new, selective acting inhibitors of serine proteases (RA-1005 and RA-1009, which are suitable targets for further structure-activity studies.

摘要

本文利用蓝藻的次生代谢产物——具有有趣生物活性的氰基肽作为新的先导结构，开展新型低分子量凝血酶抑制剂的设计、合成及抑制试验。以铜绿微囊藻毒素98 - B（1）作为先导结构，我们开发并合成了新型的、具有选择性作用的丝氨酸蛋白酶抑制剂（RA - 1005和RA - 1009），它们是进一步进行构效关系研究的合适靶点。