Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Kousei Shimada"'
Autor:
Daisuke Kozai, Nobutaka Numoto, Kouki Nishikawa, Akiko Kamegawa, Shohei Kawasaki, Yoko Hiroaki, Katsumasa Irie, Atsunori Oshima, Hiroyuki Hanzawa, Kousei Shimada, Yutaka Kitano, Yoshinori Fujiyoshi
Publikováno v:
Journal of Molecular Biology. 435:168049
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:2613-2616
The discovery and optimization of a novel series of PTHR1 antagonists are described. Starting from known PTHR1 antagonists, we identified more potent 1,4-benzodiazepin-2-one derivatives by means of a scaffold-hopping approach. The representative comp
Autor:
Kazufumi Kubota, Yuki Domon, Masayoshi Asano, Tsuyoshi Arita, Kousei Shimada, Nobuo Machinaga
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:1938-1942
We discovered a novel compound, 5-methyl-1,4,5,7-tetrahydro-2,5-ethanoazocino[4,3-b]indol-6(3H)-one sulfuric acid salt (DS39201083), which was formed by derivatization of a natural product, conolidine. DS39201083 had a unique bicyclic skeleton and wa
Autor:
Daisuke Kozai, Nobutaka Numoto, Kouki Nishikawa, Akiko Kamegawa, Shohei Kawasaki, Yoko Hiroaki, Katsumasa Irie, Atsunori Oshima, Hiroyuki Hanzawa, Kousei Shimada, Yutaka Kitano, Yoshinori Fujiyoshi
Publikováno v:
Proceedings for Annual Meeting of The Japanese Pharmacological Society. 96:1-B
Autor:
Jun Tanaka, Tsuneaki Ogata, Tsuyoshi Shinozuka, Eri Tokumaru, Nobuaki Watanabe, Satoko Wakimoto, Hideki Yamamoto, Kazushi Araki, Ryoko Sawamura, Makoto Mori, Yoshiyuki Onishi, Kunihiko Fujii, Masanori Kuroha, Yoshiro Tani, Tomoharu Tsukada, Jun Ohsumi, Kazunori Fujimoto, Kousei Shimada, Yumi Matsui
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:5079-5098
The lead identification of a novel potent selective PPARγ agonist, DS-6930 is reported. To avoid PPARγ-related adverse effects, a partial agonist was designed to prevent the direct interaction with helix 12 of PPARγ-LBD. Because the TZD group is k
Autor:
Tsuyoshi Shinozuka, Tomoharu Tsukada, Kunihiko Fujii, Eri Tokumaru, Kousei Shimada, Yoshiyuki Onishi, Yumi Matsui, Satoko Wakimoto, Masanori Kuroha, Tsuneaki Ogata, Kazushi Araki, Jun Ohsumi, Ryoko Sawamura, Nobuaki Watanabe, Hideki Yamamoto, Kazunori Fujimoto, Yoshiro Tani, Makoto Mori, Jun Tanaka
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:5099-5117
Attempts were made to reduce the lipophilicity of previously synthesized compound (II) for the avoidance of hepatotoxicity. The replacement of the left-hand side benzene with 2-pyridine resulted in the substantial loss of potency. Because poor membra
Autor:
Masayoshi Asano, Kazufumi Kubota, Yuki Domon, Kousei Shimada, Tsuyoshi Arita, Nobuo Machinaga
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(23)
We synthesized derivatives of a natural alkaloid, conolidine, and evaluated these derivatives in the acetic acid-induced writhing test and formalin test in ddY mice after oral administration. As a result, we identified (5S)-6-methyl-1,3,4,5,6,8-hexah
Autor:
Tetsuji Noguchi, Yuki Domon, Koichi Yabe, Teppei Fujimoto, Rieko Takano, Yumi Kawase, Kazufumi Kubota, Umezaki Yuma, Miki Yokoyama, Kousei Shimada, Kenjiro Ueda
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 36:127790
We identified (5R)-6-methyl-5-phenyl-1,3,4,5,6,7-hexahydro-2,5-methano-2,6-benzodiazonine (DS21980956: 4-(R)) as a novel [5.2.1]bicyclic basic compound. The scaffold was inspired by fentanyl or pethidine, which possess potent analgesic activities. DS
Autor:
Mizuki Takahashi, Kouki Nishikawa, Kousei Shimada, Akiko Kamegawa, Yoshinori Fujiyoshi, Nobutaka Numoto, Daisuke Kozai, Hiroyuki Hanzawa, Yutaka Kitano
Publikováno v:
Proceedings for Annual Meeting of The Japanese Pharmacological Society. 94:2-Y
Autor:
Masayoshi Asano, Kazufumi Kubota, Tsuyoshi Arita, Yuki Domon, Kousei Shimada, Nobuo Machinaga
Publikováno v:
Bioorganic & Medicinal Chemistry. 28:115714
We identified (5'S)-10'-fluoro-6'-methyl-5',6'-dihydro-3'H-spiro[cyclopropane-1,4'-[2,6]diaza[2,5]methano[2,6]benzodiazonin]-7'(1'H)-one, 22b (DS34942424) with a unique and original bicyclic skeleton. 22b showed an orally potent analgesic in the acet