Pyrazole-5-carboxamides, novel inhibitors of receptor for advanced glycation end products (RAGE)

…, JH Son, SJ Chung, HJ Park, J Lee, YG Suh

Index: Han, Young Taek; Kim, Kyeojin; Choi, Gyeong-In; An, Hongchan; Son, Dohyun; Kim, Hee; Ha, Hee-Jin; Son, Jun-Hyeng; Chung, Suk-Jae; Park, Hyun-Ju; Lee, Jeewoo; Suh, Young-Ger European Journal of Medicinal Chemistry, 2014 , vol. 79, p. 128 - 142

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Citation Number: 12

Abstract

Abstract In an effort to develop novel inhibitors of receptor for advanced glycation end products (RAGE) for the treatment of Alzheimer's disease, a series of pyrazole-5- carboxamides were designed, synthesized and biologically evaluated. Analyses of the extensive structure–activity relationship (SAR) led us to identify a 4-fluorophenoxy analog (40) that exhibited improved in vitro RAGE inhibitory activity and more favorable aqueous ...

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