Namoto, Kenji, Sirockin, Finton, Sellner, Holger, Wiesmann, Christian, Villard, Frederic, Valeur, Eric, Robinson, Michael, Moreau, Bob, Paulding, Stephanie, Schleeger, Simone, Schipp, Kathrin, Loup, Joachim, Andrews, Lori, 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