期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 5, 页码 906-909出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.01.064
关键词
Rhinovirus 3C protease; Protease inhibition; Covalent inhibitor; Macrocycle; Structure-based drug design; Solid phase synthesis
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. (C) 2018 Elsevier Ltd. All rights reserved.
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