{"id":11274,"date":"2022-11-22T04:55:21","date_gmt":"2022-11-21T20:55:21","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11274"},"modified":"2022-11-22T04:55:21","modified_gmt":"2022-11-21T20:55:21","slug":"ochiai-koji-et-al-published-their-research-in-bioorganic-medicinal-chemistry-letters-in-2012-cas-141032-72-6","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11274","title":{"rendered":"Ochiai, Koji et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2012 | CAS: 141032-72-6"},"content":{"rendered":"

Phosphodiesterase inhibitors. Part 4: Design, synthesis and structure-activity relationships of dual PDE3\/4-inhibitory fused bicyclic heteroaromatic-4,4-dimethylpyrazolones was written by Ochiai, Koji;Takita, Satoshi;Kojima, Akihiko;Eiraku, Tomohiko;Ando, Naoki;Iwase, Kazuhiko;Kishi, Tetsuya;Ohinata, Akira;Yageta, Yuichi;Yasue, Tokutaro;Adams, David R.;Kohno, Yasushi. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Related Products of 141032-72-6<\/a> The following contents are mentioned in the article:<\/p>\n

(-)-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-dimethylpyrazolone subunit serves as an effective surrogate for the 5-methyl-4,5-dihydropyridazin-3(2H)-one ring of KCA-1490 while lacking a stereogenic center. The 2- and 7-substituents in the pyrazolo[1,5-a]pyridine subunit markedly influence the PDE-inhibitory profile and can be adjusted to afford either potent PDE4-selective inhibitors or dual PDE3\/4 inhibitors. A survey of bicyclic heteroaromatic replacements for the pyrazolo[1,5-a]pyridine allowed further refinement of the inhibitory profile and identified 3-(8-methoxy-2-(trifluoromethyl)imidazo[1,2-a]pyridin-5-yl)-4,4-dimethyl-1H-pyrazol-5(4H)-one as an orally active, achiral KCA-1490 analog with well-balanced dual PDE3\/4-inhibitory activity. This study involved multiple reactions and reactants, such as Pyrazolo[1,5-a]pyridin-4-ol (cas: 141032-72-6Related Products of 141032-72-6<\/a>).<\/p>\n

Pyrazolo[1,5-a]pyridin-4-ol (cas: 141032-72-6) belongs to pyrazole derivatives. The strategies for the synthesis of pyrazoles generally can be applied for the construction of indazoles. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.Related Products of 141032-72-6<\/a><\/p>\n

Referemce:
Pyrazole – Wikipedia<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

Pyrazolo[1,5-a]pyridin-4-ol (cas: 141032-72-6) belongs to pyrazole derivatives. The strategies for the synthesis of pyrazoles generally can be applied for the construction of indazoles. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.Related Products of 141032-72-6<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[788,131],"tags":[128],"class_list":["post-11274","post","type-post","status-publish","format-standard","hentry","category-141032-72-6","category-pyrazoles-derivatives","tag-100-200"],"yoast_head":"\nOchiai, Koji et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2012 | CAS: 141032-72-6 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Phosphodiesterase inhibitors. Part 4: Design, synthesis and structure-activity relationships of dual PDE3\/4-inhibitory fused bicyclic heteroaromatic-4,4-dimethylpyrazolones was written by Ochiai, Koji;Takita, Satoshi;Kojima, Akihiko;Eiraku, Tomohiko;Ando, Naoki;Iwase, Kazuhiko;Kishi, Tetsuya;Ohinata, Akira;Yageta, Yuichi;Yasue, Tokutaro;Adams, David R.;Kohno, Yasushi. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Related Products of 141032-72-6 The following contents are mentioned in the article:\" \/>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/www.pyrazoles-derivatives.com\/?p=11274\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Ochiai, Koji et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2012 | CAS: 141032-72-6 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Phosphodiesterase inhibitors. Part 4: Design, synthesis and structure-activity relationships of dual PDE3\/4-inhibitory fused bicyclic heteroaromatic-4,4-dimethylpyrazolones was written by Ochiai, Koji;Takita, Satoshi;Kojima, Akihiko;Eiraku, Tomohiko;Ando, Naoki;Iwase, Kazuhiko;Kishi, Tetsuya;Ohinata, Akira;Yageta, Yuichi;Yasue, Tokutaro;Adams, David R.;Kohno, Yasushi. 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Part 4: Design, synthesis and structure-activity relationships of dual PDE3\/4-inhibitory fused bicyclic heteroaromatic-4,4-dimethylpyrazolones was written by Ochiai, Koji;Takita, Satoshi;Kojima, Akihiko;Eiraku, Tomohiko;Ando, Naoki;Iwase, Kazuhiko;Kishi, Tetsuya;Ohinata, Akira;Yageta, Yuichi;Yasue, Tokutaro;Adams, David R.;Kohno, Yasushi. 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