{"id":10046,"date":"2022-10-14T03:55:15","date_gmt":"2022-10-13T19:55:15","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10046"},"modified":"2022-10-14T03:55:15","modified_gmt":"2022-10-13T19:55:15","slug":"saito-tetsujis-team-published-research-in-bioorganic-medicinal-chemistry-in-2011-54346-19-9","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10046","title":{"rendered":"Saito, Tetsuji’s team published research in Bioorganic & Medicinal Chemistry in 2011 | 54346-19-9"},"content":{"rendered":"

Saito, Tetsuji; Obitsu, Tetsuo; Minamoto, Chiaki; Sugiura, Tsuneyuki; Matsumura, Naoya; Ueno, Sonoko; Kishi, Akihiro; Katsumata, Seishi; Nakai, Hisao; Toda, Masa-Aki published the artcile< Pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF1) receptor antagonists>, Safety of 4-Chloro-2-(methylthio)pyrazolo[1,5-a][1,3,5]triazine<\/a>, the main research area is pyrazolopyrimidine triazolopyrimidine preparation corticotropin releasing factor receptor antagonist; structure activity relationship CRF receptor antagonist pyrazolopyrimidine triazolopyrimidine.<\/p>\n

To identify structurally novel CRF1 receptor antagonists, a series of bicyclic core antagonists, pyrazolo[1,5-a]pyrimidines, e.g. I (X = CH), triazolo[1,5-a]pyrimidines, e.g. I (X = N), imidazo[1,2-a]pyrimidines, e.g. II, and a pyrazolo[1,5-a][1,3,5]triazine, III, were designed, synthesized and evaluated as CRF1 receptor antagonists. Several compounds showed binding affinity (IC50 = 4.2-418 nM) and antagonist activity (EC50 = 4.0-889 nM). Compound I (X = CH) was found to show oral efficacy in an Elevated Plus Maze test in rats. Further chem. modification of them led us to discovery of the tricyclic core antagonists pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidines, e.g. IV. The discovery process of these compounds is presented, as is the study of the structure-activity relationship.<\/p>\n

Bioorganic & Medicinal Chemistry published new progress about Aromatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 54346-19-9 belongs to class pyrazoles-derivatives, and the molecular formula is C6H5ClN4S, Safety of 4-Chloro-2-(methylthio)pyrazolo[1,5-a][1,3,5]triazine<\/a>.<\/p>\n

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

Bioorganic & Medicinal Chemistry published new progress about Aromatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 54346-19-9 belongs to class pyrazoles-derivatives, and the molecular formula is C6H5ClN4S, Safety of 4-Chloro-2-(methylthio)pyrazolo[1,5-a][1,3,5]triazine<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[751,131],"tags":[716],"class_list":["post-10046","post","type-post","status-publish","format-standard","hentry","category-54346-19-9","category-pyrazoles-derivatives","tag-m-w200-250"],"yoast_head":"\nSaito, Tetsuji's team published research in Bioorganic & Medicinal Chemistry in 2011 | 54346-19-9 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Saito, Tetsuji; Obitsu, Tetsuo; Minamoto, Chiaki; Sugiura, Tsuneyuki; Matsumura, Naoya; Ueno, Sonoko; Kishi, Akihiro; Katsumata, Seishi; Nakai, Hisao; Toda, Masa-Aki published the artcile< Pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF1) receptor antagonists>, Safety of 4-Chloro-2-(methylthio)pyrazolo[1,5-a][1,3,5]triazine, the main research area is pyrazolopyrimidine triazolopyrimidine preparation corticotropin releasing factor receptor antagonist; structure activity relationship CRF receptor antagonist pyrazolopyrimidine triazolopyrimidine.\" \/>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"http:\/\/www.pyrazoles-derivatives.com\/?p=10046\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Saito, Tetsuji's team published research in Bioorganic & Medicinal Chemistry in 2011 | 54346-19-9 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Saito, Tetsuji; Obitsu, Tetsuo; Minamoto, Chiaki; Sugiura, Tsuneyuki; Matsumura, Naoya; Ueno, Sonoko; Kishi, Akihiro; Katsumata, Seishi; Nakai, Hisao; Toda, Masa-Aki published the artcile< Pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF1) receptor antagonists>, Safety of 4-Chloro-2-(methylthio)pyrazolo[1,5-a][1,3,5]triazine, the main research area is pyrazolopyrimidine triazolopyrimidine preparation corticotropin releasing factor receptor antagonist; structure activity relationship CRF receptor antagonist pyrazolopyrimidine triazolopyrimidine.\" \/>\n<meta property=\"og:url\" content=\"http:\/\/www.pyrazoles-derivatives.com\/?p=10046\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-10-13T19:55:15+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\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=10046\",\"url\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=10046\",\"name\":\"Saito, Tetsuji's team published research in Bioorganic & Medicinal Chemistry in 2011 | 54346-19-9 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-10-13T19:55:15+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Saito, Tetsuji; Obitsu, Tetsuo; Minamoto, Chiaki; Sugiura, Tsuneyuki; Matsumura, Naoya; Ueno, Sonoko; Kishi, Akihiro; Katsumata, Seishi; Nakai, Hisao; Toda, Masa-Aki published the artcile< Pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF1) receptor antagonists>, Safety of 4-Chloro-2-(methylthio)pyrazolo[1,5-a][1,3,5]triazine, the main research area is pyrazolopyrimidine triazolopyrimidine preparation corticotropin releasing factor receptor antagonist; structure activity relationship CRF receptor antagonist pyrazolopyrimidine triazolopyrimidine.\",\"breadcrumb\":{\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=10046#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"http:\/\/www.pyrazoles-derivatives.com\/?p=10046\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=10046#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Saito, Tetsuji’s team published research in Bioorganic & Medicinal Chemistry in 2011 | 54346-19-9\"}]},{\"@type\":\"WebSite\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\",\"url\":\"https:\/\/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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