{"id":9989,"date":"2022-10-13T03:03:03","date_gmt":"2022-10-12T19:03:03","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=9989"},"modified":"2022-10-13T03:03:03","modified_gmt":"2022-10-12T19:03:03","slug":"wucherer-plietker-margaritas-team-published-research-in-bioorganic-medicinal-chemistry-letters-in-2016-cas-844501-71-9","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=9989","title":{"rendered":"Wucherer-Plietker, Margarita’s team published research in Bioorganic & Medicinal Chemistry Letters in 2016 | CAS: 844501-71-9"},"content":{"rendered":"

In 2016,Wucherer-Plietker, Margarita; Merkul, Eugen; Mueller, Thomas J. J.; Esdar, Christina; Knoechel, Thorsten; Heinrich, Timo; Buchstaller, Hans-Peter; Greiner, Hartmut; Dorsch, Dieter; Finsinger, Dirk; Calderini, Michel; Bruge, David; Graedler, Ulrich published \u300aDiscovery of novel 7-azaindoles as PDK1 inhibitors\u300b.Bioorganic & Medicinal Chemistry Letters published the findings.COA of Formula: C9H15BN2O2<\/a> The information in the text is summarized as follows:<\/p>\n

A combined screening strategy using HTS together with focused kinase library and virtual screening led to the identification of diverse chem. series as PDK1 inhibitors. The authors focused the medicinal chem. efforts on 7-azaindoles with low micromolar IC50s, e.g. I (IC50 = 1.1 \u03bcM) in the biochem. PDK1 assay. The structure-guided optimization efforts considered also PDK1 x-ray structures with weaker binding fragments and resulted in 7-azaindoles with significantly improved biochem. PDK1 potency in the two-digit nanomolar range. However, the most potent analogs only showed moderate activities in a cellular mechanistic assay, e.g. II (IC50 = 2.3 \u03bcM) together with either low microsomal stability or low permeability. The described structure-activity relationship together with PDK1 x-ray structures and early ADME data provided the basis for the subsequent hit-to-lead program. The experimental process involved the reaction of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9COA of Formula: C9H15BN2O2<\/a>)<\/p>\n

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. COA of Formula: C9H15BN2O2<\/a><\/p>\n

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

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. COA of Formula: C9H15BN2O2<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[745,131],"tags":[128],"class_list":["post-9989","post","type-post","status-publish","format-standard","hentry","category-844501-71-9","category-pyrazoles-derivatives","tag-100-200"],"yoast_head":"\nWucherer-Plietker, Margarita's team published research in Bioorganic & Medicinal Chemistry Letters in 2016 | CAS: 844501-71-9 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"In 2016,Wucherer-Plietker, Margarita; Merkul, Eugen; Mueller, Thomas J. 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J.; Esdar, Christina; Knoechel, Thorsten; Heinrich, Timo; Buchstaller, Hans-Peter; Greiner, Hartmut; Dorsch, Dieter; Finsinger, Dirk; Calderini, Michel; Bruge, David; Graedler, Ulrich published \u300aDiscovery of novel 7-azaindoles as PDK1 inhibitors\u300b.Bioorganic & Medicinal Chemistry Letters published the findings.COA of Formula: C9H15BN2O2 The information in the text is summarized as follows:\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=9989#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=9989\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=9989#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Wucherer-Plietker, Margarita’s team published research in Bioorganic & Medicinal Chemistry Letters in 2016 | CAS: 844501-71-9\"}]},{\"@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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