Synthesis, Biological Evaluation, and Molecular Modeling Studies of New Thiadiazole Derivatives as Potent P2X7 Receptor Inhibitors

Twenty new 2-(1H-pyrazol-1-yl)-1,3,4-thiadiazole analogs were synthetized to develop P2X7 receptor (P2X7R) inhibitors. P2X7R inhibition in vitro was evaluated in mouse peritoneal macrophages, HEK-293 cells transfected with hP2X7R (dye uptake assay), and THP-1 cells (IL-1β release assay). The 1-(5-ph...

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Detalles Bibliográficos
Autores principales: Gonzaga, Daniel T. G., Oliveira, Felipe H., von Ranke, N. L., Pinho, G. Q., Salles, Juliana P., Bello, Murilo L., Rodrigues, Carlos R., Castro, Helena C., de Souza, Hellen V. C. M., Reis, Caroline R. C., Leme, Rennan P. P., Mafra, João C. M., Pinheiro, Luiz C. S., Hoelz, Lucas V. B., Boechat, Nubia, Faria, Robson X.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2019
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6511888/
https://www.ncbi.nlm.nih.gov/pubmed/31134177
http://dx.doi.org/10.3389/fchem.2019.00261

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