Výsledky vyhledávání - "Kazuhiko, Iwase"

Akademický článek

Sulfonamide-based non-alkyne LpxC inhibitors as Gram-negative antibacterial agents

Autor: Kawai, Tetsuya, Kazuhiko, Iwase, Takaya, Noriko, Yamaguchi, Yuko, Kishii, Ryuta, Kohno, Yasushi, Kurasaki, Haruaki

Publikováno v: In Bioorganic & Medicinal Chemistry Letters 15 February 2017 27(4):1045-1049

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Phosphodiesterase inhibitors. Part 6: Design, synthesis, and structure–activity relationships of PDE4-inhibitory pyrazolo[1,5-a]pyridines with anti-inflammatory activity

Autor: Yuichi Yageta, Yasushi Kohno, Koji Ochiai, Satoshi Takita, Tatsunobu Sumiya, Akira Ohinata, Tokutaro Yasue, Akihiko Kojima, Kazuhiko Iwase, Tetsuya Kishi

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:5311-5316

We previously identified KCA-1490 [(−)-6-(7-methoxy-2-trifluoromethyl-pyrazolo[1,5-a]pyridin-4-yl)-5-methyl-4,5-dihydro-3-(2H)-pyridazinone], a dual PDE3/4 inhibitor. In the present study, we found highly potent selective PDE4 inhibitors derived fr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16cce9459a049b9c8c9d88786e466bde
https://doi.org/10.1016/j.bmcl.2013.07.069

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LpxC Inhibitors: Design, Synthesis, and Biological Evaluation of Oxazolidinones as Gram-negative Antibacterial Agents

Autor: Naoki Ando, Noriko Takaya, Yasushi Kohno, Kosuke Tsuda, Yuko Yamaguchi, Masahiro Nomura, Kazuhiko Iwase, Ryuta Kishii, Haruaki Kurasaki, Mariko Shinoyama

Herein we report a scaffold-hopping approach to identify a new scaffold with a zinc binding headgroup. Structural information was used to give novel oxazolidinone-based LpxC inhibitors. In particular, the most potent compound, 23j, showed a low efflu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a39016427b973359e91039c0bbcfad82
https://europepmc.org/articles/PMC4904260/

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Phosphodiesterase inhibitors. Part 2: Design, synthesis, and structure–activity relationships of dual PDE3/4-inhibitory pyrazolo[1,5-a]pyridines with anti-inflammatory and bronchodilatory activity

Autor: Koji Ochiai, David R. Adams, Hitomi Zushi, Naoki Ando, Tokutaro Yasue, Kazuhiko Iwase, Akira Ohinata, Yasushi Kohno, Tetsuya Kishi, Kazunori Fukuchi

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:5451-5456

A structural survey of pyrazolopyridine-pyridazinone phosphodiesterase (PDE) inhibitors was made with a view to optimization of their dual PDE3/4-inhibitory activity for respiratory disease applications. These studies identified (−)-6-(7-methoxy-2-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8e45d34f54d9955a24410feaa86d5169
https://doi.org/10.1016/j.bmcl.2011.06.118

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Novel nikkomycin analogues: inhibitors of the fungal cell wall biosynthesis enzyme chitin synthase

Autor: Kikoh Obi, Junichiro Uda, Osamu Sugimoto, Hiroyuki Ebisu, Kazuhiko Iwase, Akira Matsuda

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 10:1451-1454

A series of novel nikkomycin analogue inhibitors of the chitin synthase of fungal cell wall was synthesized and evaluated for their inhibitory activities. Among them, the compound having a phenanthrene group at the terminal amino acid was found to po

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b3e55ec9a85d2d56295efed707060eae
https://doi.org/10.1016/s0960-894x(00)00256-0

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[Untitled]

Autor: Kazuhiko Iwase, Shuichi Hirono

Publikováno v: Journal of Computer-Aided Molecular Design. 13:499-512

We have developed a new program, SUPERPOSE, to superpose two molecules based on the physicochemical properties of functional atoms within individual molecules. SUPERPOSE treats a pseudo-molecule consisting of functional atoms instead of a real molecu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ea8345e51112e673a283aee0b494cdac
https://doi.org/10.1023/a:1008011422113

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Phosphodiesterase inhibitors. Part 5: hybrid PDE3/4 inhibitors as dual bronchorelaxant/anti-inflammatory agents for inhaled administration

Autor: David R. Adams, Tetsuya Kishi, Tokutaro Yasue, Satoshi Takita, Tomohiko Eiraku, Yuichi Yageta, Yasushi Kohno, Koji Ochiai, Akihiko Kojima, Kazuhiko Iwase, Akira Ohinata

Publikováno v: Bioorganicmedicinal chemistry letters. 23(1)

(-)-6-(7-Methoxy-2-(trifluoromethyl)pyrazolo[1,5-a]pyridin-4-yl)-5-methyl-4,5-dihydropyridazin-3(2H)-one (KCA-1490) exhibits moderate dual PDE3/4-inhibitory activity and promises as a combined bronchodilatory/anti-inflammatory agent. N-alkylation of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f9195d96c091e790317f75dff3a576a4
https://pubmed.ncbi.nlm.nih.gov/23200255

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Phosphodiesterase inhibitors. Part 4: design, synthesis and structure-activity relationships of dual PDE3/4-inhibitory fused bicyclic heteroaromatic-4,4-dimethylpyrazolones

Autor: Tetsuya Kishi, Tomohiko Eiraku, Naoki Ando, Yuichi Yageta, Yasushi Kohno, Akihiko Kojima, David R. Adams, Satoshi Takita, Kazuhiko Iwase, Tokutaro Yasue, Koji Ochiai, Akira Ohinata

Publikováno v: Bioorganicmedicinal chemistry letters. 22(18)

(–)-6-(7-Methoxy-2-trifluoromethylpyrazolo[1,5-a]pyridin-4-yl)-5-methyl-4,5-dihydro-3-(2H)-pyridazinone (KCA-1490) is a dual PDE3/4 inhibitor that exhibits potent combined bronchodilatory and anti-inflammatory activity. Here we show that a 4,4-dime

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1de64c1b563fff6dae342bb9a1d21c51
https://pubmed.ncbi.nlm.nih.gov/22884989

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