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先导化合物结构优化策略_四_改善化合物的血脑屏障通透性

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relationships, and biological studies [J]. J Med Chem, 1999, 42: 4362 ?4379. [16] Giblin GM, Billinton A, Briggs M, et al. Discovery of 1-[4- (3-chlorophenylamino)-1-methyl-1 H-pyrrolo [3, 2-c] pyridin- 7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain rant 5-azaindole CB agonist for the treatment of chronic pain [J]. J Med Chem, 2009, 52: 5785 ?5788. [17] Shi F, Shen JK, Chen D, et al. Discovery and SAR of a series of agonists at orphan G protein-coupled receptor 139 [J]. ACS Med Chem Lett, 2011, 2: 303 ?306. [18] Ashwood VA, Field MJ, Horwell DC, et al. Utilization of an intramolecular hydrogen bond to increase S ration of an NK receptor antagonist [J]. J Med Chem, 2001, 44: 2276 ?2285. [19] Jones CK, Engers DW, Thompson AD, et al. Discovery,

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