{"id":10112,"date":"2022-10-14T07:45:02","date_gmt":"2022-10-13T23:45:02","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10112"},"modified":"2022-10-14T07:45:02","modified_gmt":"2022-10-13T23:45:02","slug":"joergensen-mortens-team-published-research-in-bioorganic-medicinal-chemistry-in-2013-cas-847818-74-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10112","title":{"rendered":"Joergensen, Morten’s team published research in Bioorganic & Medicinal Chemistry in 2013 | CAS: 847818-74-0"},"content":{"rendered":"

In 2013,Joergensen, Morten; Joergensen, Pernille N.; Christoffersen, Claus T.; Jensen, Klaus G.; Balle, Thomas; Bang-Andersen, Benny published \u300aDiscovery of novel \u03b11-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands\u300b.Bioorganic & Medicinal Chemistry published the findings.Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/a> The information in the text is summarized as follows:<\/p>\n

The synthesis and in vitro preclin. profile of a series of 5-heteroaryl substituted analogs of the antipsychotic drug sertindole are presented. Compounds 1-(4-fluorophenyl)-3-(1-methylpiperidin-4-yl)-5-(pyrimidin-5-yl)-1H-indole (Lu AA27122, 3i) and 1-(4-fluorophenyl)-5-(1-methyl-1H-1,2,4-triazol-3-yl)-3-(1-methylpiperidin-4-yl)-1H-indole (3l) were identified as high affinity \u03b11A-adrenoceptor ligands with Ki values of 0.52 and 0.16 nM, resp., and with a >100-fold selectivity vs. dopamine D2 receptors. Compound 3i showed almost equal affinity for \u03b11B- (Ki = 1.9 nM) and \u03b11D-adrenoceptors (Ki = 2.5 nM) as for \u03b11A, as well as moderate affinity for 5-HT1B (Ki = 13 nM) and 5-HT6 (Ki = 16 nM) receptors, whereas 3l showed >40-fold selectivity toward all other targets tested. Based on in vitro assays for assessment of permeability rates and extent, it is predicted that both compounds enter the brain of rats, non-human primates, as well as humans, and as such are good candidates to be carried forward for further evaluation as positron emission tomog. (PET) ligands.1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/a>) was used in this study.<\/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, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/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, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/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-10112","post","type-post","status-publish","format-standard","hentry","category-847818-74-0","category-pyrazoles-derivatives","tag-200-300"],"yoast_head":"\nJoergensen, Morten's team published research in Bioorganic & Medicinal Chemistry in 2013 | CAS: 847818-74-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"In 2013,Joergensen, Morten; Joergensen, Pernille N.; Christoffersen, Claus T.; Jensen, Klaus G.; Balle, Thomas; Bang-Andersen, Benny published \u300aDiscovery of novel \u03b11-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands\u300b.Bioorganic & Medicinal Chemistry published the findings.Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The information in the text is summarized as follows:\" \/>\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=10112\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Joergensen, Morten's team published research in Bioorganic & Medicinal Chemistry in 2013 | CAS: 847818-74-0 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"In 2013,Joergensen, Morten; Joergensen, Pernille N.; Christoffersen, Claus T.; Jensen, Klaus G.; Balle, Thomas; Bang-Andersen, Benny published \u300aDiscovery of novel \u03b11-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands\u300b.Bioorganic & Medicinal Chemistry published the findings.Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The information in the text is summarized as follows:\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=10112\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-10-13T23:45:02+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=\"2 minutes\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\/\/schema.org\",\"@graph\":[{\"@type\":\"WebPage\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10112\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10112\",\"name\":\"Joergensen, Morten's team published research in Bioorganic & Medicinal Chemistry in 2013 | CAS: 847818-74-0 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-10-13T23:45:02+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"In 2013,Joergensen, Morten; Joergensen, Pernille N.; Christoffersen, Claus T.; Jensen, Klaus G.; Balle, Thomas; Bang-Andersen, Benny published \u300aDiscovery of novel \u03b11-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands\u300b.Bioorganic & Medicinal Chemistry published the findings.Name: 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The information in the text is summarized as follows:\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10112#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=10112\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10112#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Joergensen, Morten’s team published research in Bioorganic & Medicinal Chemistry in 2013 | CAS: 847818-74-0\"}]},{\"@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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