Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors.
Bioorg Med Chem Lett
; 28(5): 906-909, 2018 03 01.
Article
in En
| MEDLINE
| ID: mdl-29433930
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.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Antiviral Agents
/
Rhinovirus
/
Viral Proteins
/
Drug Design
/
Cysteine Proteinase Inhibitors
/
Macrocyclic Compounds
Limits:
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2018
Type:
Article