{"id":12116,"date":"2023-02-02T07:35:24","date_gmt":"2023-02-01T23:35:24","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=12116"},"modified":"2023-02-02T07:35:24","modified_gmt":"2023-02-01T23:35:24","slug":"zheng-ke-et-al-published-their-research-in-journal-of-medicinal-chemistry-in-2014-cas-5334-39-4","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=12116","title":{"rendered":"Zheng, Ke et al. published their research in Journal of Medicinal Chemistry in 2014 | CAS: 5334-39-4"},"content":{"rendered":"<p>Design and Synthesis of Highly Potent and Isoform Selective JNK3 Inhibitors: SAR Studies on Aminopyrazole Derivatives was written by Zheng, Ke;Iqbal, Sarah;Hernandez, Pamela;Park, HaJeung;LoGrasso, Philip V.;Feng, Yangbo. And the article was included in Journal of Medicinal Chemistry in 2014.<a href=\"https:\/\/www.ambeed.com\/products\/5334-39-4.html\">COA of Formula: C4H5N3O2<\/a> This article mentions the following:<\/p>\n<p>The c-jun N-terminal kinase 3 (JNK3) is expressed primarily in the brain. Numerous reports have shown that inhibition of JNK3 is a promising strategy for treatment of neurodegeneration. The optimization of aminopyrazole-based JNK3 inhibitors with improved potency, isoform selectivity, and pharmacol. properties by structure-activity relationship (SAR) studies utilizing biochem. and cell-based assays, and structure-based drug design is reported. These inhibitors had high selectivity over JNK1 and p38\u03b1, minimal cytotoxicity, potent inhibition of 6-OHDA-induced mitochondrial membrane potential dissipation and ROS generation, and good drug metabolism and pharmacokinetic (DMPK) properties for iv dosing. 26n was profiled against 464 kinases and was found to be highly selective hitting only seven kinases with &gt;80% inhibition at 10 \u03bcM. Moreover, 26n showed good solubility, good brain penetration, and good DMPK properties. Finally, the crystal structure of 26k in complex with JNK3 was solved at 1.8 \u00c5 to explore the binding mode of aminopyrazole based JNK3 inhibitors. 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\">COA of Formula: C4H5N3O2<\/a>).<\/p>\n<p>3-Methyl-4-nitro-1H-pyrazole (cas: 5334-39-4) belongs to pyrazole derivatives. The strategies for the synthesis of pyrazoles generally can be applied for the construction of indazoles. The presence of both electronegative nitrogen atoms in the pyrazole ring reduces the electron density of the C3- and C5-positions leaving electron density of C4-position unaltered. Thus the C4-position is vulnerable to electrophilic attack. The C3 electrophilic-position may undergo deprotonation in the presence of a strong base leading to ring opening.<a href=\"https:\/\/www.ambeed.com\/products\/5334-39-4.html\">COA of Formula: C4H5N3O2<\/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. The strategies for the synthesis of pyrazoles generally can be applied for the construction of indazoles. The presence of both electronegative nitrogen atoms in the pyrazole ring reduces the electron density of the C3- and C5-positions leaving electron density of C4-position unaltered. Thus the C4-position is vulnerable to electrophilic attack. The C3 electrophilic-position may undergo deprotonation in the presence of a strong base leading to ring opening.<a href=\"https:\/\/www.ambeed.com\/products\/5334-39-4.html\">COA of Formula: C4H5N3O2<\/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-12116","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>Zheng, Ke et al. published their research in Journal of Medicinal Chemistry in 2014 | CAS: 5334-39-4 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Design and Synthesis of Highly Potent and Isoform Selective JNK3 Inhibitors: SAR Studies on Aminopyrazole Derivatives was written by Zheng, Ke;Iqbal, Sarah;Hernandez, Pamela;Park, HaJeung;LoGrasso, Philip V.;Feng, Yangbo. And the article was included in Journal of Medicinal Chemistry in 2014.COA of Formula: C4H5N3O2 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=12116\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Zheng, Ke et al. published their research in Journal of Medicinal Chemistry in 2014 | CAS: 5334-39-4 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Design and Synthesis of Highly Potent and Isoform Selective JNK3 Inhibitors: SAR Studies on Aminopyrazole Derivatives was written by Zheng, Ke;Iqbal, Sarah;Hernandez, Pamela;Park, HaJeung;LoGrasso, Philip V.;Feng, Yangbo. 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