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Synthesis and Evaluation of a Ruthenium-based Mitochondrial Calcium Uptake Inhibitor
Published on: October 26, 2017
Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors
Kenji Namoto1, Finton Sirockin1, Holger Sellner1
1Novartis Institutes for BioMedical Research, Novartis Campus, CH-4002 Basel, Switzerland.
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.
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