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Discovery of novel pyrrole derivatives as potent agonists for the niacin receptor GPR109A.
Miyazawa, Yuriko; Yamaguchi, Takahiro; Yamaguchi, Mitsuhiro; Tago, Keiko; Tamura, Akihiro; Sugiyama, Daisuke; Aburatani, Takahide; Nishizawa, Tomohiro; Kurikawa, Nobuya; Kono, Keita.
Afiliación
  • Miyazawa Y; External Affairs Department, Daiichi Sankyo Co., Ltd., Nihonbashi-honcho, Chuo-ku, Tokyo 103-8426, Japan. Electronic address: miyazawa.yuriko.kv@daiichisankyo.co.jp.
  • Yamaguchi T; Modality Research Laboratories, Daiichi Sankyo Co., Ltd., Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • Yamaguchi M; R&D Planning & Management Department, Daiichi Sankyo Co., Ltd., Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • Tago K; Medicinal Chemistry Research Laboratories, Daiichi Sankyo RD Novare Co., Ltd., Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • Tamura A; Organic Synthesis Department, Daiichi Sankyo RD Novare Co., Ltd., Kitakasai, Edogawa-ku, Tokyo 134-8630, Japan.
  • Sugiyama D; Drug Metabolism & Pharmacokinetics Research Laboratories, Daiichi Sankyo Co., Ltd., Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • Aburatani T; Modality Research Laboratories, Daiichi Sankyo Co., Ltd., Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • Nishizawa T; External Affairs Department, Daiichi Sankyo Co., Ltd., Nihonbashi-honcho, Chuo-ku, Tokyo 103-8426, Japan.
  • Kurikawa N; Specialty Medicine Research Laboratories II, Daiichi Sankyo Co., Ltd., Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
  • Kono K; Specialty Medicine Research Laboratories I, Daiichi Sankyo Co., Ltd., Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
Bioorg Med Chem Lett ; 30(10): 127105, 2020 05 15.
Article en En | MEDLINE | ID: mdl-32199732
ABSTRACT
Novel pyrrole derivatives were discovered as potent agonists of the niacin receptor, GPR109A. During the derivatization, compound 16 was found to be effective both in vitro and in vivo. The compound 16 exhibited a significant reduction of the non-esterified fatty acid in human GPR109A transgenic rats, and the duration of its in vivo efficacy was much longer than niacin.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Pirroles / Agonistas Nicotínicos / Receptores Acoplados a Proteínas G Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article
Texto completo
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Pirroles / Agonistas Nicotínicos / Receptores Acoplados a Proteínas G Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article