Zobrazeno 1 - 10
of 89
pro vyhledávání: '"Kazuo Sakane"'
Autor:
Kouji, Hattori, Fujiko, Takamura, Akira, Tanaka, Hisashi, Takasugi, Kiyoshi, Taniguchi, Mie, Nishio, Satoshi, Koyama, Jiro, Seki, Kazuo, Sakane
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3284-3287
A metabolism study of FR181157 (1) led to the discovery of new oxazole derivatives as active metabolites. The metabolite 6 with an epoxy ring exhibited high anti-aggregative potency with an IC(50) of 5.8 nM and potent binding affinity for the human r
Autor:
Mie Nishio, Kouji Hattori, Masahide Higaki, Jiro Seki, Satoshi Koyama, Kiyoshi Taniguchi, Osamu Okitsu, Akira Tanaka, Seiichiro Tabuchi, Kazuo Sakane
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3091-3095
The new classes of diphenylcarbamate derivatives with a tetrahydronaphthalene skeleton as highly potent and selective IP agonists have been discovered. The optimized diphenylcarbamate type compound FK-788: (R)-4 exhibited potent antiaggregative poten
Autor:
Kazuo Sakane, Satoru Kuroda, Hiromichi Itani, Atsushi Akahane, Fujiko Takamura, Yasuyo Tomishima, Yoshiyuki Tenda
Publikováno v:
CHEMICAL & PHARMACEUTICAL BULLETIN. 49:988-998
A novel series of 3-(2-substituted-3-oxo-2,3-dihydropyridazin-6-yl)-2-phenylpyrazolo[1,5-a]pyridines (5—38) were synthesized and evaluated for their in vitro adenosine A1 and A2A receptor binding activities, and in vitro metabolism by rat liver in
Publikováno v:
Japanese Journal of Pharmacology. 85:175-182
The anti-inflammatory and ulcerogenic effects of FR188582, 3-chloro-5-[4-(methylsulfonyl) phenyl]-1-phenyl-1H-pyrazole, were investigated. In a recombinant human cyclooxygenase (COX) enzyme activity, FR188582 inhibited COX-2 with an IC50 value of 0.0
Autor:
Kouji Hattori, Hirokazu Tanaka, Kazunori Tsubaki, Kazuo Sakane, Seiichiro Tabuchi, Kiyoshi Taniguchi, Osamu Okitsu, Jiro Seki
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2787-2790
A novel optically pure pyridazinone derivative was synthesized and identified as a nonprostanoid PGI 2 agonist. It inhibited ADP-induced aggregation of human platelets with an IC 50 value of 0.081 μM and has high oral bioavailability (56%) with a lo
Autor:
Tetsuo Tomishi, Hirohumi Ishikawa, Yousuke Katsura, Hisashi Takasugi, Kazuo Sakane, Yoshimi Matsumoto, Yoshikazu Inoue, Chizu Morinaga
Publikováno v:
Journal of Medicinal Chemistry. 43:3315-3321
In order to find a new class of anti-Helicobacter pylori (H. pylori) agents, a series of 4-[(3-acetamido)phenyl]-2-(substituted guanidino)thiazoles and some structurally rigid analoges were synthesized and evaluated for antimicrobial activity against
Autor:
Takeshi Terasawa, Kohji Kawabata, Hirofumi Yamamoto, Satoru Matsumoto, Shuichi Tawara, Kazuo Sakane, Ayako Nakamura, Yoshimi Matsumoto
Publikováno v:
Bioorganic & Medicinal Chemistry. 8:1159-1170
A series of 7beta-[(Z)-2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamid o]cephalosporins having a pyridine ring connected through various spacer moieties at the C-3 position was designed and synthesized and evaluated for antibacterial activity and oral
Autor:
Kazumi Otomo, Noriko Teratani, Katsuyuki Maki, Akira Yamada, Hidenori Ohki, Hisashi Takasugi, Yoshihiko Morishita, Masaki Tomishima, Hirokazu Tanaka, Fumiaki Ikeda, Koji Kawabata, Fumio Matsumoto, Shogo Kuwahara, Toshio Goto, Shuichi Tawara, Kazuo Sakane
Publikováno v:
Antimicrobial Agents and Chemotherapy. 44:57-62
The currently available antifungal drugs for the treatment of deep-seated mycoses are limited to amphotericin B (AMPH-B), azole compounds, and flucytosine. AMPH-B remains the drug of choice for the treatment of most fungal diseases because it has bro
Autor:
Kazuo Sakane, Atsushi Akahane, Satoru Kuroda, Takayoshi Kinoshita, Isao Nakanishi, Kieran Durkin, Shintaro Nishimura, Hiromichi Itani
Publikováno v:
Tetrahedron. 55:10351-10364
An efficient synthesis of FR166124 ( 1 ) was achieved through a novel sequential Horner-Emmons -isomerization reaction of cyclohexanone ( 2 ) with tert -butyl diethylphosphonoacetate ( 3 ) as the key process. Extensive studies of the key reaction ind
Autor:
Yousuke Katsura, Mitsuko Ohno, Hirohumi Ishikawa, Kazuo Sakane, Shigetaka Nishino, Chizu Morinaga, Hisashi Takasugi, Yoshimi Matsumoto
Publikováno v:
Journal of Medicinal Chemistry. 42:2920-2926
A series of 2-[(arylalkyl)guanidino]-4-[(5-acetamidomethyl)furan-2-yl]thiazole s and some 4-acetamidomethyl positional isomers were synthesized and evaluated for antimicrobial activity against Helicobacter pylori. Among the compounds that had potent