Literature DB >> 19713109

Synthesis and antiviral activity of HCV NS3/4A peptidomimetic boronic acid inhibitors.

Amogh Boloor1, Denise Hanway, Maria Joshi, David T Winn, Gabriel Mendez, Marlena Walls, Ping Wei, Fuxin Qian, Xiaoli Zhang, Yuliang Zhang, Michael E Hepperle, Xinqiang Li, David A Campbell, Juan M Betancort.   

Abstract

A new series of NS3/4A protease boronic acid inhibitors is described. The compounds show good biochemical potency and cellular activity. The peptidomimetic inhibitors were evaluated against proteases from different HCV genotypes and clinically relevant NS3/4A mutants. Compound 28 displayed subnanomolar to single digit nanomolar potencies in the enzymatic assays and an EC50 of 25 nM in the replicon cell-based assay.

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Year:  2009        PMID: 19713109     DOI: 10.1016/j.bmcl.2009.08.017

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  Design, structure-based focusing and in silico screening of combinatorial library of peptidomimetic inhibitors of Dengue virus NS2B-NS3 protease.

Authors:  Vladimir Frecer; Stanislav Miertus
Journal:  J Comput Aided Mol Des       Date:  2010-03-21       Impact factor: 3.686

Review 2.  Synthesis of biologically active boron-containing compounds.

Authors:  Fei Yang; Mingyan Zhu; Jinyi Zhang; Huchen Zhou
Journal:  Medchemcomm       Date:  2017-11-28       Impact factor: 3.597

Review 3.  Organic carbamates in drug design and medicinal chemistry.

Authors:  Arun K Ghosh; Margherita Brindisi
Journal:  J Med Chem       Date:  2015-01-07       Impact factor: 7.446

4.  A solid-phase approach for the synthesis of α-aminoboronic acid peptides.

Authors:  Blake E Daniels; Craig E Stivala
Journal:  RSC Adv       Date:  2018-01-16       Impact factor: 4.036

Review 5.  The Boron Advantage: The Evolution and Diversification of Boron's Applications in Medicinal Chemistry.

Authors:  Katia Messner; Billy Vuong; Geoffrey K Tranmer
Journal:  Pharmaceuticals (Basel)       Date:  2022-02-22
  5 in total

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