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Pyrazole-5-carboxamides, novel inhibitors of receptor for advanced glycation end products (RAGE).
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.
Afiliación
  • Han YT; College of Pharmacy, Woosuk University, Wanju 565-701, Republic of Korea.
  • Kim K; College of Pharmacy, Seoul National University, 599 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
  • Choi GI; College of Pharmacy, Seoul National University, 599 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
  • An H; College of Pharmacy, Seoul National University, 599 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
  • Son D; School of Pharmacy, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
  • Kim H; Medifron DBT, Sandanro 349, Danwon-Gu, Ansan-City, Gyeonggi-Do 425-839, Republic of Korea.
  • Ha HJ; Medifron DBT, Sandanro 349, Danwon-Gu, Ansan-City, Gyeonggi-Do 425-839, Republic of Korea.
  • Son JH; College of Pharmacy, Seoul National University, 599 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
  • Chung SJ; College of Pharmacy, Seoul National University, 599 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
  • Park HJ; School of Pharmacy, Sungkyunkwan University, Suwon 440-746, Republic of Korea.
  • Lee J; College of Pharmacy, Seoul National University, 599 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
  • Suh YG; College of Pharmacy, Seoul National University, 599 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea. Electronic address: ygsuh@snu.ac.kr.
Eur J Med Chem ; 79: 128-42, 2014 May 22.
Article en En | MEDLINE | ID: mdl-24727489
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 solubility than the parent 2-aminopyrimidine, 1. Surface plasmon resonance (SPR) and molecular docking study strongly supported the RAGE inhibitory activity of pyrazole-5-carboxamides. The brain Aß-lowering effect of 40 is also described.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Receptores Inmunológicos Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2014 Tipo del documento: Article Pais de publicación: Francia
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Receptores Inmunológicos Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2014 Tipo del documento: Article Pais de publicación: Francia