Výsledky vyhledávání - "Tomohiro, Nigo"

Syntheses of [14C]-labeled 2-(3-chlorophenyloxy)-3-[3-(3-hydroxy) pyridin-4-yl propoxy]pyridine, a phosphodiesterase 4 inhibitor and its metabolites

Autor: Takaaki Sumiyoshi, Yusuke Sawayama, Tomohiro Nigo, Motoji Kawasaki, Takeshi Ochi, Masashi Nakao, Tomoki Omodani

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 57:477-479

We describe here the synthesis of [14C]-2-(3-chlorophenyloxy)-3-[3-(3-hydroxy)pyridin-4-yl propoxy]pyridine (1), a phosphodiesterase 4 inhibitor. [14C]-Labeled 1 was prepared in three steps from [14C]-2-bromopyridin-3-ol in an overall yield of 32%. P

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3ac2ce8217117c426c3e6da72de00822
https://doi.org/10.1002/jlcr.3211

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Identification of 2,3-disubstituted pyridines as potent, non-emetic PDE4 inhibitors

Autor: Akira Fusano, Takaaki Sumiyoshi, Satoshi Matsumoto, Shunya Nakamura, Hiroshi Toda, Naruaki Nomura, Mari N. Ito, Motoji Kawasaki, Yasuhiro Teranishi, Tomohiro Nigo

Publikováno v: Bioorganicmedicinal chemistry letters. 24(12)

A series of 2,3-disubstituted pyridines were synthesized as potential non-emetic PDE4 inhibitors. To decrease brain exposure and minimize emesis, we modified the lipophilic moiety of a series of emetic PDE4 inhibitors and found that introduction of a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e18ac3b9e6cc2ba533c8e2bf6e0e2ee
https://pubmed.ncbi.nlm.nih.gov/24794103

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Syntheses of [14C]-labeled 2-(3-chlorophenyloxy)-3-[3-(3-hydroxy) pyridin-4-yl propoxy]pyridine, a phosphodiesterase 4 inhibitor and its metabolites

Autor: Takeshi, Ochi, Yusuke, Sawayama, Motoji, Kawasaki, Tomohiro, Nigo, Masashi, Nakao, Tomoki, Omodani, Takaaki, Sumiyoshi

Publikováno v: Journal of labelled compoundsradiopharmaceuticals. 57(7)

We describe here the synthesis of [(14)C]-2-(3-chlorophenyloxy)-3-[3-(3-hydroxy)pyridin-4-yl propoxy]pyridine (1), a phosphodiesterase 4 inhibitor. [(14)C]-Labeled 1 was prepared in three steps from [(14)C]-2-bromopyridin-3-ol in an overall yield of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::2691e89e3d9a481f3bea4200cca0abca
https://pubmed.ncbi.nlm.nih.gov/24966159

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Identification of 2,3-disubstituted pyridines as potent, orally active PDE4 inhibitors

Autor: Shunya Nakamura, Akira Fusano, Yasuhiro Teranishi, Tomohiro Nigo, Motoji Kawasaki, Takaaki Sumiyoshi, Mari N. Ito, Yoshihiro Kato

Publikováno v: Bioorganicmedicinal chemistry. 21(18)

A series of 2,3-disubstituted pyridines were synthesized and evaluated for their PDE4 inhibitory activity. We successfully modified undesirable cyano group of initial lead compound 2 to 4-pyridyl group with improvement of in vitro efficacy and optimi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b0ac494c5857b8e9a3bedbf53f274f7
https://pubmed.ncbi.nlm.nih.gov/23910988

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Mechanistic Study of Base-Promoted Rearrangement of 1,5-Dibromopentacyclo[5.3.0.02,5.03,9.04,8]decane-6,10-dione to 10-Oxa-9-oxopentacyclo[5.3.0.02,4.03,6.05,8]decane-3-carboxylic Acid

Autor: Yoshiyuki Kuwatani, Takeshi Hasegawa, Ikuo Ueda, Tomohiro Nigo

Publikováno v: Bulletin of the Chemical Society of Japan. 66:2676-2681

The conversion of 1,5-dibromopentacyclo[5.3.0.02,5.03,9.04,8]decane-6,10-dione (1) to 10-oxa-9-oxopentacyclo [5.3.0.02,4.03,6.05,8]decane-3-carboxylic acid (6) on treatment with 5% aqueous potassium hydroxide was shown to proceed through 1, exo-7-dib

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c9fd6845bb2846590c97fc58d52c4bb5
https://doi.org/10.1246/bcsj.66.2676

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Base-Promoted Rearrangement of 1,5-Dibromopentacyclo[5.3.0.02,5.03,9.04,8]decane-6,10-dione: Easy Entry of a Novel Cage System, 10-Oxa-9-oxopentacyclo[5.3.0.02,4.03,6.05,8]decane

Autor: Tomohiro Nigo, Takeshi Hasegawa, Ikuo Ueda, Yoshiyuki Kuwatani

Publikováno v: Bulletin of the Chemical Society of Japan. 66:2068-2072

The Diels-Alder dimerization of 2-bromo-2,4-cyclopentadienone ethylene acetal (2) gave endo-2,7-dibromodicyclopentadiene-1,8-dione 1,8-bis (ethylene acetal) (3) as a minor product in a 4.5% yield. Ultraviolet irradiation of 5 led to dimerization prod

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ff9307252ba14d464917910f48899fd6
https://doi.org/10.1246/bcsj.66.2068

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Antiulcer Agents. III. Synthesis and Antiulcer Activity of N-(3-(3-Piperidinomethylphenoxy)propyl)pentacyclo(4.2.0.02,5.03,8.04,7)octane Carboxamides and Related Compounds

Autor: Takeshi Hasegawa, Takao Kakita, Harumasa Toya, Hiromu Toyoda, Ikuo Ueda, Tomohiro Nigo

Publikováno v: Chemical and Pharmaceutical Bulletin. 41:1760-1768

The synthesis and antiulcer activity of highly strained cage compounds such as pentacyclo[4.2.0.0(2,5).0(3,8).0(4,7)]-octane (cubane), pentacyclo[4.3.0.0(2,5).0(3,8).0(4,7)]nonane (homocubane) and pentacyclo[5.3.0.0(2,4).0(3,6).0(5,8)]decane are desc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d0ae4fa815d906e02e5031db7bd66e14
https://doi.org/10.1248/cpb.41.1760

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