Novel hybrids of 1,2,3-triazole-benzoxazole: design, synthesis, and assessment of DprE1 enzyme inhibitors using fluorometric assay and computational analysis.
Triazoles
/ chemistry
Benzoxazoles
/ chemistry
Enzyme Inhibitors
/ pharmacology
Drug Design
Structure-Activity Relationship
Dose-Response Relationship, Drug
Mycobacterium tuberculosis
/ drug effects
Molecular Structure
Fluorometry
Bacterial Proteins
/ antagonists & inhibitors
Models, Molecular
Microbial Sensitivity Tests
Alcohol Oxidoreductases
/ antagonists & inhibitors
1,2,3-triazoles
DprE1 inhibitor assay
Tuberculosis
Journal
Journal of enzyme inhibition and medicinal chemistry
ISSN: 1475-6374
Titre abrégé: J Enzyme Inhib Med Chem
Pays: England
ID NLM: 101150203
Informations de publication
Date de publication:
Dec 2024
Dec 2024
Historique:
medline:
27
9
2024
pubmed:
27
9
2024
entrez:
27
9
2024
Statut:
ppublish
Résumé
Decaprenylphosphoryl-β-D-ribose-oxidase (DprE1), a subunit of the essential decaprenylphosphoribose-2'-epimerase, plays a crucial role in the synthesis of cell wall arabinan components in mycobacteria, including the pathogen responsible for tuberculosis, Identification of 15 (BOK-1–BOK-10 and BOP-1–BOP-5) potent inhibitors of DprE1 enzyme from 1,2,3-triazole ligands.BOK-2 and BOK-3 exhibited significant DprE1 inhibition with IC
Autres résumés
Type: plain-language-summary
(eng)
Identification of 15 (BOK-1–BOK-10 and BOP-1–BOP-5) potent inhibitors of DprE1 enzyme from 1,2,3-triazole ligands.BOK-2 and BOK-3 exhibited significant DprE1 inhibition with IC
Identifiants
pubmed: 39329328
doi: 10.1080/14756366.2024.2403744
doi:
Substances chimiques
Triazoles
0
Benzoxazoles
0
Enzyme Inhibitors
0
DprE1 protein, Mycobacterium tuberculosis
EC 1.1.-
Bacterial Proteins
0
Alcohol Oxidoreductases
EC 1.1.-
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM