Design, synthesis and glycosidase inhibition of DAB derivatives with C-4 peptide and dipeptide branches.
Org Biomol Chem
; 21(13): 2729-2741, 2023 03 29.
Article
en En
| MEDLINE
| ID: mdl-36916165
ABSTRACT
A series of DAB-peptide and DAB-dipeptide derivatives were synthesized from D-tartrate-derived nitrone 18. The DAB peptides 16 are derivatives of trans,trans-3,4-dihydroxy-L-proline. Glycosidase inhibition assay found four of them to be weak and selective bovine liver ß-galactosidase inhibitors, and the C-2' methyl substituted compound 23b showed the most potent ß-galactosidase inhibition (IC50 = 0.66 µM). Molecular docking studies revealed different docking modes of compound 23b compared to those of other DAB-peptides, and partial similarity of compound 23b to DGJ.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Dipéptidos
/
Glicósido Hidrolasas
Límite:
Animals
Idioma:
En
Revista:
Org Biomol Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2023
Tipo del documento:
Article
País de afiliación:
China