Hybrid molecules of scutellarein and tertramethylpyrazine's active metabolites for ischemic stroke.
Bioorg Med Chem Lett
; 29(19): 126608, 2019 10 01.
Article
en En
| MEDLINE
| ID: mdl-31444086
ABSTRACT
A series of hybrid molecules of scutellarein and tertramethylpyrazine's active metabolites have been synthesized. Compared to the original compound, these prepared compounds exhibited higher water solubility, more appropriate logP and better stability. Importantly, compounds 11b, 11d and 11e showed improved neuroprotective activity against the H2O2-induced cell death in PC12 cells, and better antithrombosis activity. The optimized compound 11b was further evaluated by cerebral ischemia/ reperfusion in the middle cerebral artery occlusion (MCAO) model, the results showed that the compound could significantly reduce the infarct area and decrease the neuronal cell damage in CA1 pyramidal neurons. Overall, we demonstrated that the twin drug strategy could be applied in the development of agents for the treatment of ischemic stroke.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Pirazinas
/
Daño por Reperfusión
/
Isquemia Encefálica
/
Fármacos Neuroprotectores
/
Accidente Cerebrovascular
/
Infarto de la Arteria Cerebral Media
/
Apigenina
Tipo de estudio:
Etiology_studies
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2019
Tipo del documento:
Article