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6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists.
Sun, Wei; Kim, Hyo-Shin; Lee, Sunho; Jung, Aeran; Kim, Sung-Eun; Ann, Jihyae; Yoon, Suyoung; Choi, Sun; Lee, Jin Hee; Blumberg, Peter M; Frank-Foltyn, Robert; Bahrenberg, Gregor; Schiene, Klaus; Stockhausen, Hannelore; Christoph, Thomas; Frormann, Sven; Lee, Jeewoo.
Afiliación
  • Sun W; Shenyang Pharmaceutical University, Shenyang 110016, China; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
  • Kim HS; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
  • Lee S; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
  • Jung A; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
  • Kim SE; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
  • Ann J; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
  • Yoon S; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
  • Choi S; National Leading Research Laboratory of Molecular Modeling & Drug Design, College of Pharmacy, Graduate School of Pharmaceutical Science and Global Top 5 Research Program, Ewha Womans University, Seoul 120-750, Republic of Korea.
  • Lee JH; National Leading Research Laboratory of Molecular Modeling & Drug Design, College of Pharmacy, Graduate School of Pharmaceutical Science and Global Top 5 Research Program, Ewha Womans University, Seoul 120-750, Republic of Korea.
  • Blumberg PM; Laboratory of Cancer Biology and Genetics, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA.
  • Frank-Foltyn R; Grunenthal Innovation, Grunenthal GmbH, D-52078 Aachen, Germany.
  • Bahrenberg G; Grunenthal Innovation, Grunenthal GmbH, D-52078 Aachen, Germany.
  • Schiene K; Grunenthal Innovation, Grunenthal GmbH, D-52078 Aachen, Germany.
  • Stockhausen H; Grunenthal Innovation, Grunenthal GmbH, D-52078 Aachen, Germany.
  • Christoph T; Grunenthal Innovation, Grunenthal GmbH, D-52078 Aachen, Germany.
  • Frormann S; Grunenthal Innovation, Grunenthal GmbH, D-52078 Aachen, Germany.
  • Lee J; Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
Bioorg Med Chem Lett ; 25(4): 803-6, 2015 Feb 15.
Article en En | MEDLINE | ID: mdl-25597011
ABSTRACT
A series of N-[{2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)-pyridin-3-yl}methyl] N'-(6,6-fused heterocyclic) ureas have been investigated as hTRPV1 antagonists. Among them, compound 15 showed highly potent TRPV1 antagonism to capsaicin, with Ki(ant)=0.2nM, as well as antagonism to other activators, and it was efficacious in a pain model. A docking study of 15 with our hTRPV1 homology model indicates that there is crucial hydrogen bonding between the ring nitrogen and the receptor, contributing to its potency.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Urea / Canales Catiónicos TRPV Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Urea / Canales Catiónicos TRPV Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article