{"id":11881,"date":"2022-12-30T07:43:12","date_gmt":"2022-12-29T23:43:12","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11881"},"modified":"2022-12-30T07:43:12","modified_gmt":"2022-12-29T23:43:12","slug":"chan-bryan-k-et-al-published-their-research-in-acs-medicinal-chemistry-letters-in-2013-cas-5334-39-4","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11881","title":{"rendered":"Chan, Bryan K. et al. published their research in ACS Medicinal Chemistry Letters in 2013 | CAS: 5334-39-4"},"content":{"rendered":"<p>Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor was written by Chan, Bryan K.;Estrada, Anthony A.;Chen, Huifen;Atherall, John;Baker-Glenn, Charles;Beresford, Alan;Burdick, Daniel J.;Chambers, Mark;Dominguez, Sara L.;Drummond, Jason;Gill, Andrew;Kleinheinz, Tracy;Le Pichon, Claire E.;Medhurst, Andrew D.;Liu, Xingrong;Moffat, John G.;Nash, Kevin;Scearce-Levie, Kimberly;Sheng, Zejuan;Shore, Daniel G.;Van de Poel, Herve;Zhang, Shuo;Zhu, Haitao;Sweeney, Zachary K.. And the article was included in ACS Medicinal Chemistry Letters in 2013.<a href=\"https:\/\/www.ambeed.com\/products\/5334-39-4.html\">SDS of cas: 5334-39-4<\/a> This article mentions the following:<\/p>\n<p>The modulation of LRRK2 kinase activity by a selective small mol. inhibitor has been proposed as a potentially viable treatment for Parkinson&#8217;s disease. By using aminopyrazoles as aniline bioisosteres, we discovered a novel series of LRRK2 inhibitors. Herein, we describe our optimization effort that resulted in the identification of a highly potent, brain-penetrant aminopyrazole LRRK2 inhibitor (18, <strong>I<\/strong>) that addressed the liabilities (e.g., poor solubility and metabolic soft spots) of our previously disclosed anilino-aminopyrimidine inhibitors. In in vivo rodent PKPD studies, 18 demonstrated good brain exposure and engendered significant reduction in brain pLRRK2 levels post-i.p. administration. The strategies of bioisosteric substitution of aminopyrazoles for anilines and attenuation of CYP1A2 inhibition described herein have potential applications to other drug discovery programs. In the experiment, the researchers used many compounds, for example, 3-Methyl-4-nitro-1H-pyrazole (cas: 5334-39-4<a href=\"https:\/\/www.ambeed.com\/products\/5334-39-4.html\">SDS of cas: 5334-39-4<\/a>).<\/p>\n<p>3-Methyl-4-nitro-1H-pyrazole (cas: 5334-39-4) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. Pyrazole the presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. <a href=\"https:\/\/www.ambeed.com\/products\/5334-39-4.html\">SDS of cas: 5334-39-4<\/a><\/p>\n<p>Referemce:<br \/><a href=\"https:\/\/en.wikipedia.org\/wiki\/Pyrazole\">Pyrazole &#8211; Wikipedia<\/a>,<br \/><a href=\"https:\/\/www.sciencedirect.com\/topics\/chemistry\/pyrazoles\">Pyrazoles &#8211; an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>3-Methyl-4-nitro-1H-pyrazole (cas: 5334-39-4) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. Pyrazole the presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. <a href=\"https:\/\/www.ambeed.com\/products\/5334-39-4.html\">SDS of cas: 5334-39-4<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[131],"tags":[128],"class_list":["post-11881","post","type-post","status-publish","format-standard","hentry","category-pyrazoles-derivatives","tag-100-200"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Chan, Bryan K. et al. published their research in ACS Medicinal Chemistry Letters in 2013 | CAS: 5334-39-4 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor was written by Chan, Bryan K.;Estrada, Anthony A.;Chen, Huifen;Atherall, John;Baker-Glenn, Charles;Beresford, Alan;Burdick, Daniel J.;Chambers, Mark;Dominguez, Sara L.;Drummond, Jason;Gill, Andrew;Kleinheinz, Tracy;Le Pichon, Claire E.;Medhurst, Andrew D.;Liu, Xingrong;Moffat, John G.;Nash, Kevin;Scearce-Levie, Kimberly;Sheng, Zejuan;Shore, Daniel G.;Van de Poel, Herve;Zhang, Shuo;Zhu, Haitao;Sweeney, Zachary K.. And the article was included in ACS Medicinal Chemistry Letters in 2013.SDS of cas: 5334-39-4 This article mentions the following:\" \/>\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=11881\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Chan, Bryan K. et al. published their research in ACS Medicinal Chemistry Letters in 2013 | CAS: 5334-39-4 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor was written by Chan, Bryan K.;Estrada, Anthony A.;Chen, Huifen;Atherall, John;Baker-Glenn, Charles;Beresford, Alan;Burdick, Daniel J.;Chambers, Mark;Dominguez, Sara L.;Drummond, Jason;Gill, Andrew;Kleinheinz, Tracy;Le Pichon, Claire E.;Medhurst, Andrew D.;Liu, Xingrong;Moffat, John G.;Nash, Kevin;Scearce-Levie, Kimberly;Sheng, Zejuan;Shore, Daniel G.;Van de Poel, Herve;Zhang, Shuo;Zhu, Haitao;Sweeney, Zachary K.. 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