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

التفاصيل البيبلوغرافية
العنوان: Synthesis and evaluation of novel α-amino cyclic boronates as inhibitors of HCV NS3 protease
المؤلفون: 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
المصدر: Bioorganic & Medicinal Chemistry Letters. 20:3550-3556
بيانات النشر: Elsevier BV, 2010.
سنة النشر: 2010
مصطلحات موضوعية: 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
الوصف: 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.
تدمد: 0960-894X
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b19b36f802cbd917e005f688fe4d445
https://doi.org/10.1016/j.bmcl.2010.04.129
حقوق: CLOSED
رقم الأكسشن: edsair.doi.dedup.....2b19b36f802cbd917e005f688fe4d445
قاعدة البيانات: OpenAIRE