{"id":10099,"date":"2022-10-14T07:45:02","date_gmt":"2022-10-13T23:45:02","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10099"},"modified":"2022-10-14T07:45:02","modified_gmt":"2022-10-13T23:45:02","slug":"liu-chunchis-team-published-research-in-european-journal-of-medicinal-chemistry-in-2016-cas-847818-74-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10099","title":{"rendered":"Liu, Chunchi&#8217;s team published research in European Journal of Medicinal Chemistry in 2016 | CAS: 847818-74-0"},"content":{"rendered":"<p><a href=\"https:\/\/www.ambeed.com\/products\/847818-74-0.html\">Quality Control of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/a>In 2016 ,\u300aDesign, synthesis and biological evaluation of novel cholesteryl ester transfer protein inhibitors bearing a cycloalkene scaffold\u300b appeared in European Journal of Medicinal Chemistry. The author of the article were Liu, Chunchi; Luo, Changqun; Hao, Lijuan; Wu, Qiong; Xie, Honglei; Zhao, Shizhen; Hao, Chenzhou; Zhao, Dongmei; Cheng, Maosheng. The article conveys some information:<\/p>\n<p>Cholesteryl ester transfer protein (CETP) is a potential target for cardiovascular disease therapy as inhibition of CETP leads to increased HDL-C in humans. Based on the structure of Merck&#8217;s biphenyl CETP inhibitor, authors designed novel N,N-substituted-cycloalkenyl-methylamine scaffold derivatives by utilizing core replacement and conformational restriction strategies. Consequently, twenty-eight compounds were synthesized and evaluated for their inhibitory activity against CETP. Their preliminary structure-activity relationships (SARs) studies indicate that polar substituents were tolerated in moiety A and hydrophobic alkyl groups at the 5-position of cyclohexene were critical for potency. Among them, compound 17a, bearing an N-(5-pyrazolyl-pyrimidin-2-yl)-cycloalkenyl- methylamine scaffold, exhibited excellent CETP inhibitory activity (IC50 = 0.07 \u03bcM) in vitro. Furthermore, it showed an acceptable pharmacokinetic profile in S-D rats and efficient HDL-C increase in high-fat fed hamsters. In the part of experimental materials, we found many familiar compounds, such as 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0<a href=\"https:\/\/www.ambeed.com\/products\/847818-74-0.html\">Quality Control of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/a>)<\/p>\n<p>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, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. <a href=\"https:\/\/www.ambeed.com\/products\/847818-74-0.html\">Quality Control of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/a><\/p>\n<p>Referemce:<br \/><a href=\"https:\/\/en.wikipedia.org\/wiki\/Pyrazole\">Pyrazole &#8211; Wikipedia<\/a>,<br \/><a href=\"https:\/\/www.sciencedirect.com\/topics\/chemistry\/pyrazoles\">Pyrazoles &#8211; an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>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, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. <a href=\"https:\/\/www.ambeed.com\/products\/847818-74-0.html\">Quality Control of 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-10099","post","type-post","status-publish","format-standard","hentry","category-847818-74-0","category-pyrazoles-derivatives","tag-200-300"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Liu, Chunchi&#039;s team published research in European Journal of Medicinal Chemistry in 2016 | CAS: 847818-74-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Quality Control of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleIn 2016 ,\u300aDesign, synthesis and biological evaluation of novel cholesteryl ester transfer protein inhibitors bearing a cycloalkene scaffold\u300b appeared in European Journal of Medicinal Chemistry. The author of the article were Liu, Chunchi; Luo, Changqun; Hao, Lijuan; Wu, Qiong; Xie, Honglei; Zhao, Shizhen; Hao, Chenzhou; Zhao, Dongmei; Cheng, Maosheng. The article conveys some information:\" \/>\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=10099\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Liu, Chunchi&#039;s team published research in European Journal of Medicinal Chemistry in 2016 | CAS: 847818-74-0 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Quality Control of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleIn 2016 ,\u300aDesign, synthesis and biological evaluation of novel cholesteryl ester transfer protein inhibitors bearing a cycloalkene scaffold\u300b appeared in European Journal of Medicinal Chemistry. The author of the article were Liu, Chunchi; Luo, Changqun; Hao, Lijuan; Wu, Qiong; Xie, Honglei; Zhao, Shizhen; Hao, Chenzhou; Zhao, Dongmei; Cheng, Maosheng. 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The author of the article were Liu, Chunchi; Luo, Changqun; Hao, Lijuan; Wu, Qiong; Xie, Honglei; Zhao, Shizhen; Hao, Chenzhou; Zhao, Dongmei; Cheng, Maosheng. 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