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磯部 義明
BBDU
特任教授

研究者情報

■ 学位
  • 薬学博士, 岐阜薬科大学, 2003年11月
■ 研究分野
  • ライフサイエンス/薬系化学、創薬科学, 創薬化学

経歴

■ 経歴
  • 2022年01月 ー 現在
    滋賀医科大学, 産学連携推進部門, 特任教授
  • 2002年10月 ー 2021年12月
    大日本住友製薬株式会社, リサーチディビジョン, 化学研究担当プロジェクトチィレクター
  • 1988年10月 ー 2002年09月
    ジャパンエナジー株式会社
  • 1987年04月 ー 1988年07月
    吉富製薬, 技術部
■ 学歴
  • 1985年04月 ー 1987年03月
    岐阜薬科大学, 大学院薬学研究科
  • 1981年04月 ー 1985年03月
    岐阜薬科大学, 薬学部, 製造薬学科

研究活動情報

■ 論文
  • Discovery of N-(6-(5-fluoro-2-(piperidin-1-yl)phenyl)pyridazin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)methanesulfonamide as a brain-permeable and metabolically stable kynurenine monooxygenase inhibitor
    Katsunori Tsuboi; Hidenori Kimura; Yoshie Nakatsuji; Momoe Kassai; Yoko Deai; Yoshiaki Isobe
    Bioorganic & Medicinal Chemistry Letters, 2021年07月15日, 査読有り
  • Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors
    Hitoshi Watanabe; Kyoji Ishida; Masanori Yamamoto; Tomokazu Nakako; Masakuni Horiguchi; Yoshiaki Isobe
    Bioorganic & Medicinal Chemistry Letters, 2021年05月15日, 査読有り
  • N-(6-phenylpyridazin-3-yl)benzenesulfonamides as highly potent, brain-permeable, and orally active kynurenine monooxygenase inhibitors
    Hidenori Kimura; Hitoshi Suda; Momoe Kassai; Mika Endo; Yoko Deai; Masahiro Yahata; Mari Miyajima; Yoshiaki Isobe
    Bioorganic & Medicinal Chemistry Letters, 2021年02月01日, 査読有り
  • Structural analysis reveals TLR7 dynamics underlying antagonism.
    Shingo Tojo; Zhikuan Zhang; Hiroyuki Matsui; Masahiro Tahara; Mitsunori Ikeguchi; Mami Kochi; Mami Kamada; Hideki Shigematsu; Akihisa Tsutsumi; Naruhiko Adachi; Takuma Shibata; Masaki Yamamoto; Masahide Kikkawa; Toshiya Senda; Yoshiaki Isobe; Umeharu Ohto; Toshiyuki Shimizu
    Nature communications, 2020年10月15日, 査読有り
  • Synthesis and pharmacological evaluation of 11-(1,6-dimethyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepines with clozapine-like receptor occupancy at dopamine D1/D2 receptor
    Hitoshi Watanabe; Kyoji Ishida; Masanori Yamamoto; Masakuni Horiguchi; Yoshiaki Isobe
    Bioorganic & Medicinal Chemistry Letters, 2020年03月01日, 査読有り
  • Synthesis and biological evaluation of novel orally available 1-phenyl-6-aminouracils containing dimethyldihydrobenzofuranol structure for the treatment of allergic skin diseases
    Masanori Tobe; Katsunori Tsuboi; Futoshi Hasegawa; Norio Fujiwara; Yoshifumi Inoue; Masakazu Isobe; Yoshiaki Isobe
    Bioorganic and Medicinal Chemistry Letters, 2016年02月15日, 査読有り, ラスト(シニア)オーサー
  • Dihydropyrrolo[2,3- d ]pyrimidines: Selective Toll-Like Receptor 9 Antagonists from Scaffold Morphing Efforts
    Manabu Watanabe; Mai Kasai; Hideyuki Tomizawa; Masamitsu Aoki; Kazuo Eiho; Yoshiaki Isobe; Shigehiro Asano
    ACS Medicinal Chemistry Letters, 2014年11月13日, 査読有り
  • Crystal structures and structure-activity relationships of imidazothiazole derivatives as IDO1 inhibitors
    Shingo Tojo; Tetsuya Kohno; Tomoyuki Tanaka; Seiji Kamioka; Yosuke Ota; Takayuki Ishii; Keiko Kamimoto; Shigehiro Asano; Yoshiaki Isobe
    ACS Medicinal Chemistry Letters, 2014年10月09日, 査読有り, ラスト(シニア)オーサー
  • Synthesis of novel benzo-fused heteroaryl derivatives as Ca 2+/calmodulin-dependent protein kinase II inhibitors
    Masafumi Komiya; Shigehiro Asano; Nobuyuki Koike; Erina Koga; Junetsu Igarashi; Shogo Nakatani; Yoshiaki Isobe
    Chemical and Pharmaceutical Bulletin, 2013年10月, 査読有り, ラスト(シニア)オーサー
  • Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility
    Tomoaki Nakamura; Hiroki Wada; Hirotaka Kurebayashi; Tom McInally; Roger Bonnert; Yoshiaki Isobe
    Bioorganic and Medicinal Chemistry Letters, 2013年02月01日, 査読有り
  • Synthesis and structure based optimization of 2-(4-phenoxybenzoyl)-5- hydroxyindole as a novel CaMKII inhibitor
    Masafumi Komiya; Shigehiro Asano; Nobuyuki Koike; Erina Koga; Junetsu Igarashi; Shogo Nakatani; Yoshiaki Isobe
    Bioorganic and Medicinal Chemistry, 2012年12月01日, 査読有り, ラスト(シニア)オーサー
  • Suzuki-Miyaura cross-coupling reaction of aryl and heteroaryl pinacol boronates for the synthesis of 2-substituted pyrimidines
    Shigehiro Asano; Seiji Kamioka; Yoshiaki Isobe
    Tetrahedron, 2012年01月07日, 査読有り, ラスト(シニア)オーサー
  • Synthesis and structure-activity relationship of tricyclic carboxylic acids as novel anti-histamines
    Katsumi Kubota; Hirotaka Kurebayashi; Hirotaka Miyachi; Masanori Tobe; Masako Onishi; Yoshiaki Isobe
    Bioorganic and Medicinal Chemistry, 2011年05月01日, 査読有り
  • Structure and activity relationship of 2-(substituted benzoyl)- hydroxyindoles as novel CaMKII inhibitors
    Masafumi Komiya; Shigehiro Asano; Nobuyuki Koike; Erina Koga; Junetsu Igarashi; Shogo Nakatani; Yoshiaki Isobe
    Bioorganic and Medicinal Chemistry Letters, 2011年03月01日, 査読有り, ラスト(シニア)オーサー
  • 5,6,7,8-Tetrahydropyrido[4,3-d]pyrimidines as novel class of potent and highly selective CaMKII inhibitors
    Shigehiro Asano; Masafumi Komiya; Nobuyuki Koike; Erina Koga; Shogo Nakatani; Yoshiaki Isobe
    Bioorganic and Medicinal Chemistry Letters, 2010年11月15日, 査読有り, ラスト(シニア)オーサー
  • Synthesis and biological evaluation of 8-oxoadenine derivatives as toll-like receptor 7 agonists introducing the antedrug concept
    Ayumu Kurimoto; Kazuki Hashimoto; Tomoaki Nakamura; Kei Norimura; Haruhisa Ogita; Haruo Takaku; Roger Bonnert; Tom McInally; Hiroki Wada; Yoshiaki Isobe
    Journal of Medicinal Chemistry, 2010年04月08日, 査読有り, ラスト(シニア)オーサー
  • Synthesis and structure-activity relationships of phenothiazine carboxylic acids having pyrimidine-dione as novel histamine H1 antagonists
    Katsumi Kubota; Hirotaka Kurebayashi; Hirotaka Miyachi; Masanori Tobe; Masako Onishi; Yoshiaki Isobe
    Bioorganic and Medicinal Chemistry Letters, 2009年05月15日, 査読有り
  • Synthesis and biological evaluation of novel 9-substituted-8-hydroxyadenine derivatives as potent interferon inducers
    Yoshiaki Isobe; Ayumu Kurimoto; Masanori Tobe; Kazuki Hashimoto; Tomoaki Nakamura; Kei Norimura; Haruhisa Ogita; Haruo Takaku
    Journal of Medicinal Chemistry, 2006年03月23日, 査読有り
  • Prodrugs of 9-benzyl-8-hydroxy-2-(2-hydroxyethylthio)adenine: Potent interferon inducing agents in monkeys
    Ayumu Kurimoto; Masanori Tobe; Haruhisa Ogita; Tetsuhiro Ogino; Haruo Takaku; Shinji Ichii; Hajime Kawakami; Yoshiaki Isobe
    Chemical and Pharmaceutical Bulletin, 2004年04月, 査読有り, ラスト(シニア)オーサー
  • Synthesis and evaluation of 2-substituted 8-hydroxyadenines as potent interferon inducers with improved oral bioavailabilities
    Ayumu Kurimoto; Tetsuhiro Ogino; Shinji Ichii; Yoshiaki Isobe; Masanori Tobe; Haruhisa Ogita; Haruo Takaku; Hironao Sajiki; Kosaku Hirota; Hajime Kawakami
    Bioorganic and Medicinal Chemistry, 2004年03月01日, 査読有り
  • Synthesis of pyrimidine derivatives possessing an antioxidative property and their inhibitory effects on picryl chloride-induced contact hypersensitivity reaction
    Yoshiaki Isobe; Kosaku Hirota
    Chemical and Pharmaceutical Bulletin, 2003年12月, 査読有り, 筆頭著者
  • Synthesis and structure-activity relationships of 2-amino-8- hydroxyadenines as orally active interferon inducing agents
    Ayumu Kurimoto; Tetsuhiro Ogino; Shinji Ichii; Yoshiaki Isobe; Masanori Tobe; Haruhisa Ogita; Haruo Takaku; Hironao Sajiki; Kosaku Hirota; Hajime Kawakami
    Bioorganic and Medicinal Chemistry, 2003年12月01日, 査読有り
  • Structure and activity relationships of novel uracil derivatives as topical anti-inflammatory agents
    Yoshiaki Isobe; Masanori Tobe; Yoshifumi Inoue; Masakazu Isobe; Masami Tsuchiya; Hideya Hayashi
    Bioorganic and Medicinal Chemistry, 2003年11月17日, 査読有り, 筆頭著者
  • A novel structural class of potent inhibitors of NF-κB activation: Structure-activity relationships and biological effects of 6-aminoquinazoline derivatives
    Masanori Tobe; Yoshiaki Isobe; Hideyuki Tomizawa; Takahiro Nagasaki; Hirotada Takahashi; Hideya Hayashi
    Bioorganic and Medicinal Chemistry, 2003年09月01日, 査読有り
  • Synthesis and structure-activity relationships of 2-substituted-8-hydroxyadenine derivatives as orally available interferon inducers without emetic side effects
    Y Isobe; M Tobe; H Ogita; A Kurimoto; T Ogino; H Kawahami; H Takaku; H Sajiki; K Hirota; H Hayashi
    Bioorganic and Medicinal Chemistry, 2003年08月, 査読有り, 筆頭著者
  • Synthesis of potent and selective inhibitors against the proliferation of human coronary artery smooth muscle cells
    Haruhisa Ogita; Yoshiaki Isobe; Haruo Takaku; Rena Sekine; Yuso Goto; Satoru Misawa; Hideya Hayashi
    Chemical and Pharmaceutical Bulletin, 2003年02月, 査読有り
  • Discovery of quinazolines as a novel structural class of potent inhibitors of NF-κB activation
    Masanori Tobe; Yoshiaki Isobe; Hideyuki Tomizawa; Takahiro Nagasaki; Hirotada Takahashi; Tominaga Fukazawa; Hideya Hayashi
    Bioorganic and Medicinal Chemistry, 2003年02月, 査読有り
  • Synthesis and evaluation of 6-nitro-7-(1-piperazino)quinazolines: Dual-acting compounds with inhibitory activities toward both tumor necrosis factor-α (TNF-α) production and T cell proliferation
    Masanori Tobe; Yoshiaki Isobe; Hideyuki Tomizawa; Takahiro Nagasaki; Masamitsu Aoki; Toru Negishi; Hideya Hayashi
    Chemical and Pharmaceutical Bulletin, 2003年, 査読有り
  • Inhibitory activities of novel pyrimidine derivatives on the contact hypersensitivity reaction
    Yoshiaki Isobe; Masanori Tobe; Yoshifumi Inoue; Yuso Goto; Fumihiro Obara; Masakazu Isobe; Hideya Hayashi
    Chemical and Pharmaceutical Bulletin, 2003年, 査読有り, 筆頭著者
  • Discovery of 8-hydroxyadenines as a novel type of interferon inducer
    Kosaku Hirota; Kazunori Kazaoka; Itaru Niimoto; Hiroshi Kumihara; Hironao Sajiki; Yoshiaki Isobe; Haruo Takaku; Masanori Tobe; Haruhisa Ogita; Tetsuhiro Ogino; Shinji Ichii; Ayumu Kurimoto; Hajime Kawakami
    Journal of Medicinal Chemistry, 2002年12月05日, 査読有り
  • Synthesis and structure-activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human endothelial cells
    Haruhisa Ogita; Yoshiaki Isobe; Haruo Takaku; Rena Sekine; Yuso Goto; Satoru Misawa; Hideya Hayashi
    Bioorganic and Medicinal Chemistry, 2002年11月, 査読有り
  • Synthesis and activity of a metabolite of (S)-6-amino-5-(6-hydroxy-2,5,7,8- tetramethylchroman-2-carboxamido)-3-methyl-1-phenyl-2,4-(1H,3H)-pyrimidinedione (CX-659S)
    Yoshiaki Isobe; Masanori Tobe; Osamu Takahashi; Yuso Goto; Yoshifumi Inoue; Fumihiro Obara; Masami Tsuchiya; Hideya Hayashi
    Chemical and Pharmaceutical Bulletin, 2002年10月, 査読有り, 筆頭著者
  • Structure-activity relationships of 6-nitroquinazolines: Dual-acting compounds with inhibitory activities toward both TNF- α production and T cell proliferation
    Masanori Tobe; Yoshiaki Isobe; Hideyuki Tomizawa; Takahiro Nagasaki; Fumihiro Obara; Mitsuhiro Matsumoto; Hideya Hayashi
    Chemical and Pharmaceutical Bulletin, 2002年08月, 査読有り
  • Structure-activity relationships of 6-fluoroquinazolines: Dual-Acting compounds with inhibitory activities toward both TNF-α production and T cell proliferation
    Masanori Tobe; Yoshiaki Isobe; Hideyuki Tomizawa; Takahiro Nagasaki; Fumihiro Obara; Hideya Hayashi
    Bioorganic and Medicinal Chemistry, 2002年02月, 査読有り
  • Synthesis and structure-activity relationship of diarylamide urea derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells
    Haruhisa Ogita; Yoshiaki Isobe; Haruo Takaku; Rena Sekine; Yuso Goto; Satoru Misawa; Hideya Hayashi
    Bioorganic and Medicinal Chemistry, 2002年, 査読有り
  • Synthesis and structure-activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells
    Haruhisa Ogita; Yoshiaki Isobe; Haruo Takaku; Rena Sekine; Yuso Goto; Satoru Misawa; Hideya Hayashi
    Bioorganic and Medicinal Chemistry Letters, 2001年02月26日, 査読有り
  • Structure-activity relationships of quinazoline derivatives: Dual-acting compounds with inhibitory activities toward both TNF-α production and T cell proliferation
    Masanori Tobe; Yoshiaki Isobe; Hideyuki Tomizawa; Mitsuhiro Matsumoto; Fumihiro Obara; Takahiro Nagasaki; Hideya Hayashi
    Bioorganic and Medicinal Chemistry Letters, 2001年02月26日, 査読有り
  • Synthesis and biological evaluation of CX-659S and its related compounds for their inhibitory effects on the delayed-type hypersensitivity reaction
    Masanori Tobe; Yoshiaki Isobe; Yuso Goto; Fumihiro Obara; Masami Tsuchiya; Junko Matsui; Kosaku Hirota; Hideya Hayashi
    Bioorganic and Medicinal Chemistry, 2000年08月, 査読有り
  • Cloning of cDNA for rat eosinophil major basic protein
    Takeaki Nittoh; Masako Watanabe; Hiroshi Okayama; Satoru Misawa; Yoshiaki Isobe; Hideya Hayashi; Suetsugu Mue; Kazuo Ohuchi
    BBA - Gene Structure and Expression, 1995年12月27日, 査読有り
  • Facile Synthesis of Thymidine Derivatives by Cross-Coupling of 5-Halogenouridine Derivatives with Trimethylaluminum
    Kosaku Hirota; Yukio Kitade; Yoshitake Kanbe; Yoshiaki Isobe; Yukio Kitade; Yoshifumi Maki
    Synthesis, 1993年, 査読有り
  • Palladium-catalyzed cross-coupling reaction of trialkylaluminiums with aryl triflates: facile conversion of a phenolic hydroxy group into an alkyl group
    Kosaku Hirota; Yoshiaki Isobe; Yoshifumi Maki
    J. Chem. Soc., Perkin Trans. I, 1989年, 査読有り
  • Palladium catalyzed coupling of-5-hydroxyuracil trifluoromethanesulfonates with alkenes and alkynes
    Kosaku Hirota; Yukio Kitade; Yoshiaki Isobe; Yoshifumi Maki
    Heterocycles, 1987年, 査読有り
  • A Simple Synthesis of 5-(1-Alkenyl)uracil Derivatives by Palladium-Catalyzed Oxidative Coupling of Uracils With Olefins
    Kosaku Hirota; Yoshiaki Isobe; Yukio Kitade; Yoshifumi Maki
    Synthesis, 1987年, 査読有り
■ MISC
  • Synthesis and structure-activity relationships of 8-hydroxyadenines as interferon inducers.
    A Kurimoto; T Ogino; H Kawakami; Y Isobe; H Takaku; H Sajiki; K Hirota
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2002年08月, 査読無し, 通常論文