基于结构的大环人鼻病毒3C蛋白酶抑制剂的设计与合成。
Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors.
作者信息
Namoto Kenji, Sirockin Finton, Sellner Holger, Wiesmann Christian, Villard Frederic, Moreau Robert J, Valeur Eric, Paulding Stephanie C, Schleeger Simone, Schipp Kathrin, Loup Joachim, Andrews Lori, Swale Ryann, Robinson Michael, Farady Christopher J
机构信息
Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
出版信息
Bioorg Med Chem Lett. 2018 Mar 1;28(5):906-909. doi: 10.1016/j.bmcl.2018.01.064. Epub 2018 Feb 1.
The design and synthesis of macrocyclic inhibitors of human rhinovirus 3C protease is described. A macrocyclic linkage of the P1 and P3 residues, and the subsequent structure-based optimization of the macrocycle conformation and size led to the identification of a potent biochemical inhibitor 10 with sub-micromolar antiviral activity.
本文描述了人鼻病毒3C蛋白酶大环抑制剂的设计与合成。P1和P3残基的大环连接，以及随后基于结构对大环构象和大小的优化，导致鉴定出一种具有亚微摩尔抗病毒活性的强效生化抑制剂10。
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