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Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors

Namoto, Kenji and Sirockin, Finton and Sellner, Holger and Wiesmann, Christian and Villard, Frederic and Valeur, Eric and Robinson, Michael and Moreau, Bob and Paulding, Stephanie and Schleeger, Simone and Schipp, Kathrin and Loup, Joachim and Andrews, Lori and O'Neill, Ryann and Farady, Christopher (2018) Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors. Bioorganic and Medicinal Chemistry Letters, 28 (5). pp. 906-909. ISSN 14643405

Abstract

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.

Item Type: Article
Keywords: Covalent inhibitor Macrocycle Protease inhibition Rhinovirus 3C protease Solid phase synthesis Structure-based drug design
Date Deposited: 21 Mar 2018 00:45
Last Modified: 25 Jan 2019 00:45
URI: https://oak.novartis.com/id/eprint/34470

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