{"id":10088,"date":"2022-10-14T07:44:21","date_gmt":"2022-10-13T23:44:21","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10088"},"modified":"2022-10-14T07:44:21","modified_gmt":"2022-10-13T23:44:21","slug":"xu-guozhangs-team-published-research-in-bioorganic-medicinal-chemistry-letters-in-2020-cas-844501-71-9","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10088","title":{"rendered":"Xu, Guozhang’s team published research in Bioorganic & Medicinal Chemistry Letters in 2020 | CAS: 844501-71-9"},"content":{"rendered":"

\u300aHit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor\u300b was written by Xu, Guozhang; Gaul, Michael D.; Liu, Zhijie; DesJarlais, Renee L.; Qi, Jenson; Wang, Weixue; Krosky, Daniel; Petrounia, Ioanna; Milligan, Cynthia M.; Hermans, An; Lu, Hua-Rong; Huang, Devine Zheng; Xu, June Zhi; Spurlino, John C.. Recommanded Product: 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/a> And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020. The article conveys some information:<\/p>\n

G-protein coupled receptor kinase 2 (GRK2), which is upregulated in the failing heart, appears to play a critical role in heart failure (HF) progression in part because enhanced GRK2 activity promotes dysfunction of \u03b2-adrenergic signaling and myocyte death. An orally bioavailable GRK2 inhibitor could offer unique therapeutic outcomes that cannot be attained by current heart failure treatments that directly target GPCRs or angiotensin-converting enzyme. Herein, we describe the discovery of a potent, selective, and orally bioavailable GRK2 inhibitor, 8h, through high-throughput screening, hit-to-lead optimization, structure-based design, mol. modeling, synthesis, and biol. evaluation. In the cellular target engagement assays, 8h enhances isoproterenol-mediated cyclic adenosine 3′,5′-monophosphate (cAMP) production in HEK293 cells overexpressing GRK2. Compound 8h was further evaluated in a human stem cell-derived cardiomyocyte (HSC-CM) contractility assay and potentiated isoproterenol-induced beating rate in HSC-CMs. In the experiment, the researchers used 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Recommanded Product: 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/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, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Recommanded Product: 3-(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":"

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, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Recommanded Product: 3-(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":[745,131],"tags":[128],"class_list":["post-10088","post","type-post","status-publish","format-standard","hentry","category-844501-71-9","category-pyrazoles-derivatives","tag-100-200"],"yoast_head":"\nXu, Guozhang's team published research in Bioorganic & Medicinal Chemistry Letters in 2020 | CAS: 844501-71-9 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"\u300aHit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor\u300b was written by Xu, Guozhang; Gaul, Michael D.; Liu, Zhijie; DesJarlais, Renee L.; Qi, Jenson; Wang, Weixue; Krosky, Daniel; Petrounia, Ioanna; Milligan, Cynthia M.; Hermans, An; Lu, Hua-Rong; Huang, Devine Zheng; Xu, June Zhi; Spurlino, John C.. Recommanded Product: 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020. 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