Synthesis of 2,4-dihydroxyacetophenone derivatives as potent PDE-1 and -3 inhibitors: in vitro and in silico insights.
Future Med Chem
; 16(12): 1185-1203, 2024.
Article
em En
| MEDLINE
| ID: mdl-38989989
ABSTRACT
Aim:
Synthesis of novel bis-Schiff bases having potent inhibitory activity against phosphodiesterase (PDE-1 and -3) enzymes, potentially offering therapeutic implications for various conditions.Methods:
Bis-Schiff bases were synthesized by refluxing 2,4-dihydroxyacetophenone with hydrazine hydrate, followed by treatment of substituted aldehydes with the resulting hydrazone to obtain the product compounds. After structural confirmation, the compounds were screened for their in vitro PDE-1 and -3 inhibitory activities.Results:
The prepared compounds exhibited noteworthy inhibitory efficacy against PDE-1 and -3 enzymes by comparing with suramin standard. To clarify the binding interactions between the drugs, PDE-1 and -3 active sites, molecular docking studies were carried out.Conclusion:
The potent compounds discovered in this study may be good candidates for drug development.
[Box see text].
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Acetofenonas
/
Inibidores de Fosfodiesterase
/
Nucleotídeo Cíclico Fosfodiesterase do Tipo 1
/
Simulação de Acoplamento Molecular
Limite:
Humans
Idioma:
En
Revista:
Future Med Chem
Ano de publicação:
2024
Tipo de documento:
Article
País de afiliação:
Paquistão
País de publicação:
Reino Unido