{"id":10170,"date":"2022-10-17T09:11:19","date_gmt":"2022-10-17T01:11:19","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10170"},"modified":"2022-10-17T09:11:19","modified_gmt":"2022-10-17T01:11:19","slug":"emmerich-juliettes-team-published-research-in-journal-of-medicinal-chemistry-in-2017-cas-847818-74-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10170","title":{"rendered":"Emmerich, Juliette’s team published research in Journal of Medicinal Chemistry in 2017 | CAS: 847818-74-0"},"content":{"rendered":"

Application of 847818-74-0<\/a>In 2017 ,\u300aLead Optimization Generates CYP11B1 Inhibitors of Pyridylmethyl Isoxazole Type with Improved Pharmacological Profile for the Treatment of Cushing’s Disease\u300b appeared in Journal of Medicinal Chemistry. The author of the article were Emmerich, Juliette; van Koppen, Chris J.; Burkhart, Jens L.; Hu, Qingzhong; Siebenbuerger, Lorenz; Boerger, Carsten; Scheuer, Claudia; Laschke, Matthias W.; Menger, Michael D.; Hartmann, Rolf W.. The article conveys some information:<\/p>\n

Cushing’s disease, characterized by elevated plasma cortisol levels, can be controlled by inhibition of 11\u03b2-hydroxylase (CYP11B1). The previously identified selective and potent CYP11B1 inhibitor 5-((5-methylpyridin-3-yl)methyl)-2-phenylpyridine Ref 7 (IC50= 2 nM) exhibited promutagenic potential as well as very low oral bioavailability in rats (F = 2%) and was therefore modified to overcome these drawbacks. Successful lead optimization resulted in similarly potent and selective 5-((5-methoxypyridin-3-yl)methyl)-3-phenylisoxazole 25 (IC50 = 2 nM, 14-fold selectivity over CYP11B2), exhibiting a superior pharmacol. profile with no mutagenic potential. Furthermore, compound 25 inhibited rat CYP11B1 (IC50 = 2 \u03bcM) and showed a high oral bioavailability (F = 50%) and sufficient plasma concentrations in rats, providing an excellent starting point for a proof-of-principle study. After reading the article, we found that the author used 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Application of 847818-74-0<\/a>)<\/p>\n

1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Application of 847818-74-0<\/a><\/p>\n

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

1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Application of 847818-74-0<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[744,131],"tags":[129],"class_list":["post-10170","post","type-post","status-publish","format-standard","hentry","category-847818-74-0","category-pyrazoles-derivatives","tag-200-300"],"yoast_head":"\nEmmerich, Juliette's team published research in Journal of Medicinal Chemistry in 2017 | CAS: 847818-74-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Application of 847818-74-0In 2017 ,\u300aLead Optimization Generates CYP11B1 Inhibitors of Pyridylmethyl Isoxazole Type with Improved Pharmacological Profile for the Treatment of Cushing's Disease\u300b appeared in Journal of Medicinal Chemistry. The author of the article were Emmerich, Juliette; van Koppen, Chris J.; Burkhart, Jens L.; Hu, Qingzhong; Siebenbuerger, Lorenz; Boerger, Carsten; Scheuer, Claudia; Laschke, Matthias W.; Menger, Michael D.; Hartmann, Rolf W.. 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The author of the article were Emmerich, Juliette; van Koppen, Chris J.; Burkhart, Jens L.; Hu, Qingzhong; Siebenbuerger, Lorenz; Boerger, Carsten; Scheuer, Claudia; Laschke, Matthias W.; Menger, Michael D.; Hartmann, Rolf W.. 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The author of the article were Emmerich, Juliette; van Koppen, Chris J.; Burkhart, Jens L.; Hu, Qingzhong; Siebenbuerger, Lorenz; Boerger, Carsten; Scheuer, Claudia; Laschke, Matthias W.; Menger, Michael D.; Hartmann, Rolf W.. 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