Výsledky vyhledávání - "Toshihiko Nishiyama"

Discovery of new orally active prostaglandin D2 receptor antagonists

Autor: Yoko Matsunaga, Seiji Ogawa, Hisao Nakai, Yutaka Okada, Atsushi Shimabukuro, Kohki Tsukamoto, Fumio Nambu, Atsushi Kinoshita, Rie Oumi, Yoshihiko Odagaki, Ryoji Matsumoto, Atsushi Naganawa, Jun Katagi, Maki Iwahashi, Koji Yano, Masaaki Toda, Toshihiko Nishiyama, Kousuke Tani

Publikováno v: Bioorganic & Medicinal Chemistry. 19:6935-6948

To identify an orally available drug candidate, a series of 3-benzoylaminophenylacetic acids were synthesized and evaluated as prostaglandin D2 (PGD2) receptor antagonists. Some of the compounds tested were found to exhibit excellent inhibitory activ

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ee81d7e76196c761d039147212cacff
https://doi.org/10.1016/j.bmc.2011.08.065

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Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite

Autor: Kenji Maeda, Shiro Shibayama, Katsuya Hisaichi, Hideaki Tada, Yoshikazu Takaoka, Chiaki Minamoto, Toshihiko Nishiyama, Kenji Sagawa, Hiromu Habashita, Masaaki Toda, Rena Nishizawa, Naoki Matsunaga, Daikichi Fukushima, Hiroaki Mitsuya

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 17:727-731

Hydroxylated derivatives were designed and synthesized based on the information of oxidative metabolites. Compounds derived from β-substituted (2 R ,3 R )-2-amino-3-hydroxypropionic acid showed improved inhibitory activities against the binding of M

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a34de678841801760d15dffedee756f
https://doi.org/10.1016/j.bmcl.2006.10.084

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Design and Synthesis of Orally Bioavailable Inhibitors of Inducible Nitric Oxide Synthase. Identification of 2-Azabicyclo[4.1.0]heptan-3-imines

Autor: Yshihiko Odagaki, Atsuko Fujii, Toshihiko Nishiyama, Masaaki Toda, Masaharu Komeno, Hisao Nakai, Tadashi Tatsumi, Masayuki Murota, Katsuya Hisaichi, Kaoru Kobayashi, Keisuke Hirai, Masao Naka, Yasufumi Kawanaka, Shinya Kusuda

Publikováno v: Bioorganic & Medicinal Chemistry. 11:1723-1743

Further chemical modification of 2-iminopiperidines fused to cyclopropane rings was performed. Optically active isomers 2 and 13 were synthesized and their biological activity was evaluated. Compound 2 exhibited greater potency and more isoform selec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf6c329f779b701700aaf7c3eb13d7e6
https://doi.org/10.1016/s0968-0896(03)00034-8

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Design and synthesis of orally bioavailable inhibitors of inducible nitric oxide synthase. synthesis and biological evaluation of dihydropyridin-2(1H)-imines and 1,5,6,7-Tetrahydro-2H-azepin-2-imines

Autor: Masao Naka, Katsuya Hisaichi, Atsuko Fujii, Masayuki Murota, Hisao Nakai, Tadashi Tatsumi, Keisuke Hirai, Minoru Nishizaki, Yasufumi Kawanaka, Masaharu Komeno, Kaoru Kobayashi, Masaaki Toda, Toshihiko Nishiyama, Shinya Kusuda

Publikováno v: Bioorganic & Medicinal Chemistry. 11:689-702

The process of discovery and biological evaluation of alpha,beta-unsaturated cyclic amidines, as selective inhibitors of inducible nitric oxide synthase (iNOS), is reported. Dihydropyridin-2(1H)-imines and 1,5,6,7-tetrahydro-2H-azepin-2-imines were s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38a8fdc315d2193b0543032426489230
https://doi.org/10.1016/s0968-0896(02)00540-0

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Studies on novel and chiral 1,4-dihydropyridines. IV. Mechanistic aspects of the asymmetric reduction with chiral NADH model compounds, (S)-3-(p-tolylsulfinyl)-1,4-dihydropyridines

Autor: Takeshi Imanishi, Toshihiko Nishiyama, Satoshi Obika, S. Tatematsu, Kazuyuki Miyashita

Publikováno v: Tetrahedron. 53:3073-3082

In the reduction of ketones with NADH mimics, ( S S )-1-substituted 3-( p -tolylsulfinyl)-1,4-dihydropyridines 1 , the stereospecific transfer of one of the C-4 hydrogens, which is syn to the SO bond, was experimentally revealed to be involved by

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::549af78078928ec1337729044115df10
https://doi.org/10.1016/s0040-4020(97)00072-0

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Studies on novel and chiral 1,4-dihydropyridines. III. Asymmetric reduction of some ketones with novel NADH model compounds, (S)-3-(p-Tolylsulfinyl)-1,4-dihydropyridines

Autor: Takeshi Imanishi, Chuzo Iwata, Toshihiko Nishiyama, Satoshi Obika, Kazuyuki Miyashita, S. Tatematsu

Publikováno v: Tetrahedron. 53:593-602

The reactions of the novel NADH model compounds 2 with methyl benzoylformate and some other ketonic compounds were studied. The 3-( p -tolylsulfinyl) derivaties 2 successfully reduced methyl bezoylformate to give methyl ( R )-mandelate in good chemic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cb7b5a9ba060c0642161c9078e8726f2
https://doi.org/10.1016/s0040-4020(96)01005-8

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Studies on Novel and Chiral 1,4-Dihydropyridines. I. Synthesis and Conformational Analysis of Novel NADH Model Compounds, N-Substituted (S)-3-(p-Tolylsulfinyl)-1,4-dihydropyridines

Autor: Takeshi Imanishi, Yoshimitsu Hamano, Kazuyuki Miyashita, Chuzo Iwata, Satoshi Obika, M. Nishimoto, Toshihiko Nishiyama

Publikováno v: Chemical and Pharmaceutical Bulletin. 44:267-272

Novel NADH model compounds, (SS)-1-alkyl-3-(p-tolylsulfinyl)-1, 4-dihydropyridines (2) and (RS)-1-benzyl-3-[1-oxo-2-(p-tolylsulfinyl)ethyl]-1, 4-dihydropyridine (3), were synthesized. 1H-NMR study and X-ray analysis of 2 revealed its preferred confor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::dac3f36c0e6628009285de3eed46377d
https://doi.org/10.1248/cpb.44.267

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