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, 15 Jul. 2021, Refereed

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, 15 May 2021, Refereed

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, 01 Feb. 2021, Refereed

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, 15 Oct. 2020, Refereed

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, 01 Mar. 2020, Refereed

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, 15 Feb. 2016, Refereed, Last

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, 13 Nov. 2014, Refereed

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, 09 Oct. 2014, Refereed, Last

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, Oct. 2013, Refereed, Last

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, 01 Feb. 2013, Refereed

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, 01 Dec. 2012, Refereed, Last

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, 07 Jan. 2012, Refereed, Last

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, 01 May 2011, Refereed

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, 01 Mar. 2011, Refereed, Last

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, 15 Nov. 2010, Refereed, Last

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, 08 Apr. 2010, Refereed, Last

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, 15 May 2009, Refereed

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, 23 Mar. 2006, Refereed

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, Apr. 2004, Refereed, Last

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, 01 Mar. 2004, Refereed

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, Dec. 2003, Refereed, Lead

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, 01 Dec. 2003, Refereed

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, 17 Nov. 2003, Refereed, Lead

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, 01 Sep. 2003, Refereed

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, Aug. 2003, Refereed, Lead

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, Feb. 2003, Refereed

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, Feb. 2003, Refereed

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, Refereed

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, Refereed, Lead

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, 05 Dec. 2002, Refereed

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, Nov. 2002, Refereed

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, Oct. 2002, Refereed, Lead

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, Aug. 2002, Refereed

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, Feb. 2002, Refereed

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, Refereed

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, 26 Feb. 2001, Refereed

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, 26 Feb. 2001, Refereed

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, Aug. 2000, Refereed

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, 27 Dec. 1995, Refereed

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, Refereed

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, Refereed

Palladium catalyzed coupling of-5-hydroxyuracil trifluoromethanesulfonates with alkenes and alkynes
Kosaku Hirota; Yukio Kitade; Yoshiaki Isobe; Yoshifumi Maki
Heterocycles, 1987, Refereed

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, Refereed

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, Aug. 2002, Not refereed, Not invited