Fluorovinylsulfones and -Sulfonates as Potent Covalent Reversible Inhibitors of the Trypanosomal Cysteine Protease Rhodesain: Structure-Activity Relationship, Inhibition Mechanism, Metabolism, and In Vivo Studies.
Animals
Cysteine Endopeptidases
/ chemistry
Cysteine Proteinase Inhibitors
/ chemical synthesis
Enzyme Assays
Female
HeLa Cells
Humans
Kinetics
Male
Mice
Molecular Docking Simulation
Molecular Structure
Parasitic Sensitivity Tests
Protein Binding
Structure-Activity Relationship
Sulfones
/ chemical synthesis
Sulfonic Acids
/ chemical synthesis
Trypanocidal Agents
/ chemical synthesis
Trypanosoma brucei brucei
/ drug effects
Vinyl Compounds
/ chemical synthesis
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
26 08 2021
26 08 2021
Historique:
pubmed:
12
8
2021
medline:
16
11
2021
entrez:
11
8
2021
Statut:
ppublish
Résumé
Rhodesain is a major cysteine protease of
Identifiants
pubmed: 34378914
doi: 10.1021/acs.jmedchem.1c01002
doi:
Substances chimiques
Cysteine Proteinase Inhibitors
0
Sulfones
0
Sulfonic Acids
0
Trypanocidal Agents
0
Vinyl Compounds
0
Cysteine Endopeptidases
EC 3.4.22.-
rhodesain
EC 3.4.22.-
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM