Ligand-based design, synthesis, and biological evaluation of 2-aminopyrimidines, a novel series of receptor for advanced glycation end products (RAGE) inhibitors

…, D Son, NJ Kim, H Yun, S Lee, DJ Chang…

文献索引：Han, Young Taek; Choi, Gyeong-In; Kim, Nam-Jung; Yun, Hwayoung; Lee, Sujin; Chang, Dong Jo; Lee, Jeewoo; Suh, Young-Ger; Son, Dohyun; Park, Hyun-Ju; Hong, Hyun-Seok; Kim, Hee; Ha, Hee-Jin; Kim, Young-Ho Journal of Medicinal Chemistry, 2012 , vol. 55, # 21 p. 9120 - 9135,16 Title/Abstract Full Text Show Details Han, Young Taek; Choi, Gyeong-In; Son, Dohyun; Kim, Nam-Jung; Yun, Hwayoung; Lee, Sujin; Chang, Dong Jo; Hong, Hyun-Seok; Kim, Hee; Ha, Hee-Jin; Kim, Young-Ho; Park, Hyun-Ju; Lee, Jeewoo; Suh, Young-Ger Journal of Medicinal Chemistry, 2012 , vol. 55, # 21 p. 9120 - 9135

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被引用次数: 21

摘要

Using the approach of ligand-based drug design, we discovered a novel series of 4, 6- disubstituted 2-aminopyrimidines as RAGE inhibitors. In transgenic mouse models of AD, one of the 4, 6-bis (4-chlorophenyl) pyrimidine analogs, 59, significantly lowered the concentration of toxic soluble Aβ in the brain and improved cognitive function. SPR analysis confirmed the direct binding of 59 with RAGE, which should contribute to its biological ...