Structure–activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activators

X Xing, LC Chang, Q Kong, CK Colton, L Lai…

文献索引：Xing, Xuechao; Chang, Ling-Chu; Kong, Qiongman; Colton, Craig K.; Lai, Liching; Glicksman, Marcie A.; Lin, Chien-Liang Glenn; Cuny, Gregory D. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 19 p. 5774 - 5777

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被引用次数: 25

摘要

Excitatory amino acid transporter 2 (EAAT2) is the major glutamate transporter and functions to remove glutamate from synapses. A thiopyridazine derivative has been found to increase EAAT2 protein levels in astrocytes. A structure–activity relationship study revealed that several components of the molecule were required for activity, such as the thioether and pyridazine. Modification of the benzylthioether resulted in several derivatives (7-13, 7-15 ...