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Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2018 Mar 01; Vol. 28 (5), pp. 906-909. Date of Electronic Publication: 2018 Feb 01. - Publication Year :
- 2018
-
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.<br /> (Copyright © 2018 Elsevier Ltd. All rights reserved.)
- Subjects :
- 3C Viral Proteases
Antiviral Agents chemical synthesis
Antiviral Agents chemistry
Crystallography, X-Ray
Cysteine Endopeptidases metabolism
Cysteine Proteinase Inhibitors chemical synthesis
Cysteine Proteinase Inhibitors chemistry
Dose-Response Relationship, Drug
Humans
Macrocyclic Compounds chemical synthesis
Macrocyclic Compounds chemistry
Microbial Sensitivity Tests
Models, Molecular
Molecular Conformation
Rhinovirus enzymology
Structure-Activity Relationship
Viral Proteins metabolism
Antiviral Agents pharmacology
Cysteine Proteinase Inhibitors pharmacology
Drug Design
Macrocyclic Compounds pharmacology
Rhinovirus drug effects
Viral Proteins antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 28
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 29433930
- Full Text :
- https://doi.org/10.1016/j.bmcl.2018.01.064