新型α-氨基环状硼酸酯的合成与评价及其作为 HCV NS3 蛋白酶抑制剂的研究。
Synthesis and evaluation of novel alpha-amino cyclic boronates as inhibitors of HCV NS3 protease.
机构信息
Anacor Pharmaceuticals, Inc., Palo Alto, CA 94303, USA.
出版信息
Bioorg Med Chem Lett. 2010 Jun 15;20(12):3550-6. doi: 10.1016/j.bmcl.2010.04.129. Epub 2010 May 20.
PMID:20493689
Abstract
We have designed and synthesized a novel series of alpha-amino cyclic boronates and incorporated them successfully in several acyclic templates at the P1 position. These compounds are inhibitors of the HCV NS3 serine protease, and structural studies show that they inhibit the NS3 protease by trapping the Ser-139 hydroxyl group in the active site. Synthetic methodologies and SARs of this series of compounds are described.
摘要
我们设计并合成了一系列新型的α-氨基环状硼酸酯，并成功地将其引入到几个无环模板的 P1 位置。这些化合物是 HCV NS3 丝氨酸蛋白酶的抑制剂，结构研究表明它们通过将 Ser-139 羟基捕获在活性部位来抑制 NS3 蛋白酶。本文描述了这一系列化合物的合成方法和 SAR。
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