设计和合成靶向凝血级联因子 XIa 的大环吲哚。
Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa.
机构信息
Department of Chemistry, Université de Montréal, Montréal, QC, Canada.
出版信息
Bioorg Med Chem Lett. 2010 Dec 1;20(23):6925-8. doi: 10.1016/j.bmcl.2010.09.141. Epub 2010 Oct 8.
PMID:21035339
Abstract
The synthesis of a series of novel macrocyclic compounds designed to target blood coagulation Factor XIa is described. The compounds were evaluated for their inhibition of a small set of serine proteases. Several compounds displayed modest activity and good selectivity for Factor XIa. Within the series, a promising lead structure for developing novel macrocyclic inhibitors of thrombin was identified.
摘要
本文描述了一系列旨在靶向血液凝固因子 XIa 的新型大环化合物的合成。评估了这些化合物对一小部分丝氨酸蛋白酶的抑制作用。几种化合物表现出对因子 XIa 的适度活性和良好选择性。在该系列中，确定了一种有前途的用于开发新型血栓素大环抑制剂的先导结构。
Zotero 插件