{"id":11655,"date":"2022-12-01T06:40:04","date_gmt":"2022-11-30T22:40:04","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11655"},"modified":"2022-12-01T06:40:04","modified_gmt":"2022-11-30T22:40:04","slug":"liang-juns-team-published-research-in-journal-of-medicinal-chemistry-in-56-cas-763120-58-7","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11655","title":{"rendered":"Liang, Jun’s team published research in Journal of Medicinal Chemistry in 56 | CAS: 763120-58-7"},"content":{"rendered":"

Liang, Jun published the artcileLead Optimization of a 4-Aminopyridine Benzamide Scaffold To Identify Potent, Selective, and Orally Bioavailable TYK2 Inhibitors<\/i><\/b>, Synthetic Route of 763120-58-7<\/a>, the publication is Journal of Medicinal Chemistry (2013), 56(11), 4521-4536, database is CAplus and MEDLINE.<\/p>\n

Herein the authors report the authors’ lead optimization effort to identify potent, selective, and orally bioavailable TYK2 inhibitors, starting with lead mol. 2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide. The authors used structure-based design to discover 2,6-dichloro-4-cyanophenyl and (1R,2R)-2-fluorocyclopropylamide modifications, each of which exhibited improved TYK2 potency and JAK1 and JAK2 selectivity relative to 2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide. Further optimization eventually led to 2-Chloro-4-cyano-6-fluoro-N-(2-((1R,2R)-2-fluorocyclopropanecarboxamido)pyridin-4-yl)benzamide that showed good TYK2 enzyme and interleukin-12 (IL-12) cell potency, as well as acceptable cellular JAK1 and JAK2 selectivity and excellent oral exposure in mice. When tested in a mouse IL-12 PK\/PD model, 2-Chloro-4-cyano-6-fluoro-N-(2-((1R,2R)-2-ffluorocyclopropanecarboxamido)pyridin-4-yl)benzamide showed statistically significant knockdown of cytokine interferon-\u03b3 (IFN\u03b3), suggesting that selective inhibition of TYK2 kinase activity might be sufficient to block the IL-12 pathway in vivo.<\/p>\n

Journal of Medicinal Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Synthetic Route of 763120-58-7<\/a>.<\/p>\n

Referemce:
https:\/\/en.wikipedia.org\/wiki\/Pyrazole<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

Journal of Medicinal Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Synthetic Route of 763120-58-7<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[802,131],"tags":[732],"class_list":["post-11655","post","type-post","status-publish","format-standard","hentry","category-763120-58-7","category-pyrazoles-derivatives","tag-m-w100-150"],"yoast_head":"\nLiang, Jun's team published research in Journal of Medicinal Chemistry in 56 | CAS: 763120-58-7 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Liang, Jun published the artcileLead Optimization of a 4-Aminopyridine Benzamide Scaffold To Identify Potent, Selective, and Orally Bioavailable TYK2 Inhibitors, Synthetic Route of 763120-58-7, the publication is Journal of Medicinal Chemistry (2013), 56(11), 4521-4536, database is CAplus and MEDLINE.\" \/>\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=11655\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Liang, Jun's team published research in Journal of Medicinal Chemistry in 56 | CAS: 763120-58-7 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Liang, Jun published the artcileLead Optimization of a 4-Aminopyridine Benzamide Scaffold To Identify Potent, Selective, and Orally Bioavailable TYK2 Inhibitors, Synthetic Route of 763120-58-7, the publication is Journal of Medicinal Chemistry (2013), 56(11), 4521-4536, database is CAplus and MEDLINE.\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=11655\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-11-30T22:40:04+00:00\" \/>\n<meta name=\"author\" content=\"Jessica.F\" \/>\n<meta name=\"twitter:card\" content=\"summary_large_image\" \/>\n<meta name=\"twitter:label1\" content=\"Written by\" \/>\n\t<meta name=\"twitter:data1\" content=\"Jessica.F\" \/>\n\t<meta name=\"twitter:label2\" content=\"Est. reading time\" \/>\n\t<meta name=\"twitter:data2\" content=\"1 minute\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\/\/schema.org\",\"@graph\":[{\"@type\":\"WebPage\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11655\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11655\",\"name\":\"Liang, Jun's team published research in Journal of Medicinal Chemistry in 56 | CAS: 763120-58-7 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-11-30T22:40:04+00:00\",\"author\":{\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Liang, Jun published the artcileLead Optimization of a 4-Aminopyridine Benzamide Scaffold To Identify Potent, Selective, and Orally Bioavailable TYK2 Inhibitors, Synthetic Route of 763120-58-7, the publication is Journal of Medicinal Chemistry (2013), 56(11), 4521-4536, database is CAplus and MEDLINE.\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11655#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=11655\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11655#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"http:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Liang, Jun’s team published research in Journal of Medicinal Chemistry in 56 | CAS: 763120-58-7\"}]},{\"@type\":\"WebSite\",\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/#website\",\"url\":\"http:\/\/www.pyrazoles-derivatives.com\/\",\"name\":\"pyrazoles-derivatives\",\"description\":\"Several pyrazole derivatives possess important pharmacological activities and they have been proved useful materials in drug research. 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