التفاصيل البيبلوغرافية
| العنوان: |
m-Terphenylamines, Acting as Selective COX-1 Inhibitors, Block Microglia Inflammatory Response and Exert Neuroprotective Activity |
| المؤلفون: |
Damiano Rocchi, Juan F. González, Olmo Martín-Cámara, Maria Grazia Perrone, Morena Miciaccia, Antonio Scilimati, Celine Decouty-Pérez, Esther Parada, Javier Egea, J. Carlos Menéndez |
| المصدر: |
Molecules; Volume 28; Issue 14; Pages: 5374 |
| بيانات النشر: |
Multidisciplinary Digital Publishing Institute |
| سنة النشر: |
2023 |
| المجموعة: |
MDPI Open Access Publishing |
| مصطلحات موضوعية: |
terphenylamines, COX-1 inhibitors, neuroinflammation, oxidative stress, neuroprotection |
| جغرافية الموضوع: |
agris |
| الوصف: |
Inhibition of cyclooxygenase-2 (COX-2) has been extensively studied as an approach to reduce proinflammatory markers in acute brain diseases, but the anti-neuroinflammatory role of cyclooxygenase-1 (COX-1) inhibition has been rather neglected. We report that m-terphenylamine derivatives are selective COX-1 inhibitors, able to block microglia inflammatory response and elicit a neuroprotective effect. These compounds were synthesized via a three-component reaction of chalcones, β-ketoesters, and primary amines, followed by hydrolysis/decarboxylation of the ester group. Together with their synthetic intermediates and some urea derivatives, they were studied as inhibitors of COX-1 and COX-2. The m-terphenylamine derivatives, which were selective COX-1 inhibitors, were also analyzed for their ability to block microglia inflammatory and oxidative response. Compound 3b presented an interesting anti-inflammatory and neuroprotective profile by reducing nitrite release, ROS overproduction, and cell death in organotypic hippocampal cultures subjected to LPS. We thus show that COX-1 inhibition is a promising approach to provide enhanced neuroprotection against acute inflammatory processes, which are crucial in the development of a plethora of acute neurodegenerative injuries. |
| نوع الوثيقة: |
text |
| وصف الملف: |
application/pdf |
| اللغة: |
English |
| العلاقة: |
Medicinal Chemistry; https://dx.doi.org/10.3390/molecules28145374Test |
| DOI: |
10.3390/molecules28145374 |
| الإتاحة: |
https://doi.org/10.3390/molecules28145374Test |
| حقوق: |
https://creativecommons.org/licenses/by/4.0Test/ |
| رقم الانضمام: |
edsbas.B6B77F84 |
| قاعدة البيانات: |
BASE |
