Synthesis and evaluation of novel α-amino cyclic boronates as inhibitors of HCV NS3 protease

Autor:	Zhi-Jie Ni, Qun Li, Martin John Slater, Wuxin Zou, Linos Lazarides, Yang Liu, Lois L. Wright, Paul Rowland, Liang Liao, Charles Z. Ding, Tadeusz Skarzynski, Jacob J. Plattner, Jackie E. Mordaunt, Don O. Somers, Xianfeng Li, Colin M. Edge, Yong-Kang Zhang, Gemma Victoria White, Malcolm Ellis, Jon Wright, Stephen J. Baker, Dazhong Fan, Wieslaw M. Kazmierski, Gary K. Smith, Pia Thommes, Lewis E. Pennicott, Julia A. Hubbard, Richard L. Jarvest, Bill McDowell, Yasheen Zhou, Xuelei Qian, Pamela Nassau, Richard Martin Grimes
Rok vydání:	2010
Předmět:	Stereochemistry viruses medicine.medical_treatment Clinical Biochemistry Pharmaceutical Science Peptide Hepacivirus Viral Nonstructural Proteins Biochemistry Chemical synthesis Structure-Activity Relationship Catalytic Domain Drug Discovery Serine medicine Molecular Biology chemistry.chemical_classification Serine protease NS3 Protease Molecular Structure biology Organic Chemistry virus diseases Active site Boronic Acids digestive system diseases Protease inhibitor (biology) chemistry Enzyme inhibitor Drug Design biology.protein Molecular Medicine medicine.drug
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 20:3550-3556
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b19b36f802cbd917e005f688fe4d445 https://doi.org/10.1016/j.bmcl.2010.04.129 Zobrazit plný text záznamu Full Text from ScienceDirect