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

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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Bibliographic Details
Main Authors: Daniel T. G. Gonzaga, Felipe H. Oliveira, N. L. von Ranke, G. Q. Pinho, Juliana P. Salles, Murilo L. Bello, Carlos R. Rodrigues, Helena C. Castro, Hellen V. C. M. de Souza, Caroline R. C. Reis, Rennan P. P. Leme, João C. M. Mafra, Luiz C. S. Pinheiro, Lucas V. B. Hoelz, Nubia Boechat, Robson X. Faria
Format: Article
Language:English
Published: Frontiers Media S.A. 2019-04-01
Series:Frontiers in Chemistry
Subjects:
P2X7 receptor
thiadiazole
pyrazole
dye uptake
IL-1β release
paw edema
Online Access:https://www.frontiersin.org/article/10.3389/fchem.2019.00261/full

Internet

https://www.frontiersin.org/article/10.3389/fchem.2019.00261/full

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