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Design, Synthesis, and Monoamine Oxidase B Selective Inhibitory Activity of N-Arylated Heliamine Analogues.
Yamada, Makito; Hirose, Yu; Lin, Bangzhong; Fumimoto, Megumi; Nunomura, Kazuto; Natchanun, Sirimangkalakitti; Takahashi, Naoyuki; Ohki, Yuuta; Sako, Makoto; Murai, Kenichi; Harada, Kazuo; Arai, Masayoshi; Suzuki, Sayo; Nakamura, Tomonori; Haruta, Junichi; Arisawa, Mitsuhiro.
Afiliación
  • Yamada M; Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
  • Hirose Y; Graduate School of Pharmaceutical Sciences, Keio University, Shibakoen 1-5-30, Minato-ku, Tokyo 105-8512, Japan.
  • Lin B; Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
  • Fumimoto M; Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
  • Nunomura K; Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
  • Natchanun S; Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
  • Takahashi N; Tokyo Rikakikai Co. Ltd (Brand: EYELA), TN Koishikawa Bldg, 1-15-17 Koishikawa Bunkyo-ku, Tokyo 112-0002, Japan.
  • Ohki Y; Tokyo Rikakikai Co. Ltd (Brand: EYELA), TN Koishikawa Bldg, 1-15-17 Koishikawa Bunkyo-ku, Tokyo 112-0002, Japan.
  • Sako M; Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
  • Murai K; Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
  • Harada K; Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
  • Arai M; Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
  • Suzuki S; Graduate School of Pharmaceutical Sciences, Keio University, Shibakoen 1-5-30, Minato-ku, Tokyo 105-8512, Japan.
  • Nakamura T; Graduate School of Pharmaceutical Sciences, Keio University, Shibakoen 1-5-30, Minato-ku, Tokyo 105-8512, Japan.
  • Haruta J; Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
  • Arisawa M; Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
ACS Med Chem Lett ; 13(10): 1582-1590, 2022 Oct 13.
Article en En | MEDLINE | ID: mdl-36262392
Monoamine oxidase B (MAO-B) metabolizes monoamines such as dopamine regarding neural transmission and controls its level in the mammalian's brain. When MAO-B metabolizes dopamine abnormally, normal neurotransmission does not occur, and central nervous system disorders such as Parkinson's disease may develop. Although several MAO inhibitors have been developed, most of them have no selectivity between monoamine oxidase A (MAO-A) and MAO-B, or they work irreversibly against the enzyme. This report describes the first case of screening of N-arylated heliamine derivatives to develop novel MAO-B selective inhibitors that can be synthesized concisely by microwave-assisted Pd nanoparticle-catalyzed Buchwald-Hartwig amination. We discovered that the derivatives 4h, 4i, and 4j display inhibitory activity against MAO-B with IC50 values of 1.55, 13.5, and 5.08 µM, respectively.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2022 Tipo del documento: Article País de afiliación: Japón Pais de publicación: Estados Unidos
Texto completo
Añadir a Mi BVS
Imprimir
XML
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2022 Tipo del documento: Article País de afiliación: Japón Pais de publicación: Estados Unidos