| Autor: |
de Souza, Márcia Maria, Andreolla, Marina Corrêa, Ribeiro, Thaís Cecília, Gonçalves, Ana Elisa, Medeiros, Alex Rogério, de Souza, Anacleto Silva, Ferreira, Leonardo Luiz Gomes, Andricopulo, Adriano Defini, Yunes, Rosendo Augusto, de Oliveira, Aldo Sena |
| Zdroj: |
MedChemComm; 2020, Vol. 11 Issue: 2 p307-316, 10p |
| Abstrakt: |
Five synthetic sulfonamides derived from carvacrol, a natural product and a small molecule with druglike properties, were evaluated with respect to their effects on the cognitive deficits of animals with streptozotocin (STZ)-induced Alzheimer's disease (AD). Memory, ambulation, anxiety and oxidative stress were evaluated. In vitroassays were performed to assess the inhibition of acetylcholinesterase (AChE), and the data were combined with molecular docking for the establishment of structure–activity relationships. The memories of animals treated with the compounds derived from morpholine (1), hydrazine (3) and 2-phenol (5) were improved. Compound 3was the most promising, yielding excellent results in the inhibitory avoidance test. Moreover, the compounds did not exhibit any deleterious effects on the animals' ambulation in the open field test. Molecular docking confirmed the results obtained in the AChE inhibition assay. In short, compounds 1, 3and 5can reduce STZ-induced deficits and show potential for the treatment of Alzheimer's. In addition, these agents produce significant anxiolytic and antioxidant effects. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
|
