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4-Substituted carbamazepine derivatives: Conformational analysis and sodium channel-blocking properties.
Kanase, Yuki; Kitada, Takafumi; Tabata, Hidetsugu; Makino, Kosho; Oshitari, Tetsuta; Ohashi, Hiromi; Yoshinaga, Takashi; Natsugari, Hideaki; Takahashi, Hideyo.
Afiliación
  • Kanase Y; Faculty of Pharma Sciences, Teikyo University, 2-11-1, Kaga, Itabashi-ku, Tokyo 173-8605, Japan.
  • Kitada T; Faculty of Pharma Sciences, Teikyo University, 2-11-1, Kaga, Itabashi-ku, Tokyo 173-8605, Japan.
  • Tabata H; Faculty of Pharma Sciences, Teikyo University, 2-11-1, Kaga, Itabashi-ku, Tokyo 173-8605, Japan.
  • Makino K; Faculty of Pharma Sciences, Teikyo University, 2-11-1, Kaga, Itabashi-ku, Tokyo 173-8605, Japan.
  • Oshitari T; Faculty of Pharma Sciences, Teikyo University, 2-11-1, Kaga, Itabashi-ku, Tokyo 173-8605, Japan.
  • Ohashi H; Preclinical Safety Research Unit, Tsukuba R&D Supporting Division, Sunplanet Co., Ltd., 5-1-3 Tokodai, Tsukuba, Ibaraki, Japan.
  • Yoshinaga T; Global Cardiovascular Assessment, Biopharmaceutical Assessment Core Function Unit, Medicine Development Center, Eisai Co., Ltd., 5-1-3 Tokodai, Tsukuba, Ibaraki, Japan.
  • Natsugari H; Faculty of Pharma Sciences, Teikyo University, 2-11-1, Kaga, Itabashi-ku, Tokyo 173-8605, Japan.
  • Takahashi H; Faculty of Pharma Sciences, Teikyo University, 2-11-1, Kaga, Itabashi-ku, Tokyo 173-8605, Japan. Electronic address: hide-tak@pharm.teikyo-u.ac.jp.
Bioorg Med Chem ; 26(9): 2508-2513, 2018 05 15.
Article en En | MEDLINE | ID: mdl-29673716
ABSTRACT
The physicochemical properties of 4-substituted carbamazepine derivatives were investigated. It was elucidated that the 4-substitution is not effective in reducing the rotations (E/Z) about the N-C1' axes around the outer carbamoyl moiety. However, the atropisomers were isolated with high stereochemical stability, meaning that the 4-substitution reduced the butterfly motion of the tricyclic ring system efficiently. The Cl/CH3-substituted carbamazepine derivatives showed greater inhibitory effects on hNav1.2 channel currents compared with carbamazepine, although no difference in the activity between enantiomers was observed.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Carbamazepina / Bloqueadores de los Canales de Sodio / Canal de Sodio Activado por Voltaje NAV1.2 Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: Japón
Texto completo
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Carbamazepina / Bloqueadores de los Canales de Sodio / Canal de Sodio Activado por Voltaje NAV1.2 Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: Japón