Novel benzimidazole derivatives as effective inhibitors of prolyl oligopeptidase: synthesis, in vitro and in silico analysis.
Future Med Chem
; 16(1): 43-58, 2024 Jan.
Article
em En
| MEDLINE
| ID: mdl-38054466
ABSTRACT
Background:
This research aims to discover novel derivatives having potential therapeutic applications in treating conditions related to prolyl oligopeptidase (POP) dysfunction.Method:
Novel benzimidazole derivatives have been synthesized, characterized and screened for their in vitro POP inhibition.Results:
All these derivatives showed excellent-to-good inhibitory activities in the range of IC50 values of 3.61 ± 0.15 to 43.72 ± 1.18 µM, when compared with standard Z-prolyl-prolinal. The docking analysis revealed the strong interactions between our compounds and the target enzyme, providing critical insights into their binding affinities and potential implications for drug development.Conclusion:
The significance of these compounds in targeting POP enzyme offers promising prospects for future research in the field of neuropharmacology.Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Serina Endopeptidases
/
Prolil Oligopeptidases
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article