Optimization of a small tropomyosin-related kinase B (TrkB) agonist 7, 8-dihydroxyflavone active in mouse models of depression

X Liu, CB Chan, Q Qi, G Xiao, HR Luo…

文献索引：Liu, Xia; Chan, Chi-Bun; Qi, Qi; Ye, Keqiang; Xiao, Ge; Luo, Hongbo R.; He, Xiaolin Journal of Medicinal Chemistry, 2012 , vol. 55, # 19 p. 8524 - 8537,14

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被引用次数: 37

摘要

Structure–activity relationship study shows that the catechol group in 7, 8-dihdyroxyflavone, a selective small TrkB receptor agonist, is critical for agonistic activity. To improve the poor pharmacokinetic profiles intrinsic to catechol-containing molecules and to elevate the agonistic effect of the lead compound, we initiated the lead optimization campaign by synthesizing various bioisosteric derivatives. Here we show that the optimized 2-methyl-8- ...