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- ...
[Hamid, M. Haniti S. A.; Allen, C. Liana; Lamb, Gareth W.; Maxwell, Aoife C.; Maytum, Hannah C.; et al. Journal of the American Chemical Society, 2009 , vol. 131, p. 1766 - 1774]
