| Title | Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors. | ||
| Author | Namoto, Kenji; Sirockin, Finton; Sellner, Holger; Wiesmann, Christian; Villard, Frederic; Moreau, Robert J; Valeur, Eric; Paulding, Stephanie C; Schleeger, Simone; Schipp, Kathrin; Loup, Joachim; Andrews, Lori; Swale, Ryann; Robinson, Michael; Farady, Christopher J | ||
| Journal | Bioorg Med Chem Lett | Publication Year/Month | 2018-Mar |
| PMID | 29433930 | PMCID | -N/A- |
| Affiliation + expend | 1.Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland. Electronic address: kenji.namoto@novartis.com. | ||
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.