{"id":11796,"date":"2022-12-05T02:37:14","date_gmt":"2022-12-04T18:37:14","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11796"},"modified":"2022-12-05T02:37:14","modified_gmt":"2022-12-04T18:37:14","slug":"reiberger-roberts-team-published-research-in-international-journal-of-molecular-sciences-in-22-cas-724710-02-5","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11796","title":{"rendered":"Reiberger, Robert’s team published research in International Journal of Molecular Sciences in 22 | CAS: 724710-02-5"},"content":{"rendered":"

Reiberger, Robert published the artcileSynthesis and In Vitro Evaluation of C-7 and C-8 Luteolin Derivatives as Influenza Endonuclease Inhibitors<\/i><\/b>, Synthetic Route of 724710-02-5<\/a>, the publication is International Journal of Molecular Sciences (2021), 22(14), 7735, database is CAplus and MEDLINE.<\/p>\n

The part of the influenza polymerase PA subunit featuring endonuclease activity is a target for anti-influenza therapies, including the FDA-approved drug Xofluza. A general feature of endonuclease inhibitors is their ability to chelate Mg2+<\/sup> or Mn2+<\/sup> ions located in the enzyme\u2032s catalytic site. Previously, we screened a panel of flavonoids for PA inhibition and found luteolin and its C-glucoside orientin to be potent inhibitors. Through structural anal., we identified the presence of a 3\u2032,4\u2032-dihydroxyphenyl moiety as a crucial feature for sub-micromolar inhibitory activity. Here, we report results from a subsequent investigation exploring structural changes at the C-7 and C-8 positions of luteolin. Exptl. IC50<\/sub> values were determined by AlphaScreen technol. The most potent inhibitors were C-8 derivatives with inhibitory potencies comparable to that of luteolin. Bio-isosteric replacement of the C-7 hydroxyl moiety of luteolin led to a series of compounds with one-order-of-magnitude-lower inhibitory potencies. Using X-ray crystallog., we solved structures of the wild-type PA-N-terminal domain and its I38T mutant in complex with orientin at 1.9 \u00c5 and 2.2 \u00c5 resolution, resp.<\/p>\n

International Journal of Molecular Sciences published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Synthetic Route of 724710-02-5<\/a>.<\/p>\n

Referemce:
https:\/\/en.wikipedia.org\/wiki\/Pyrazole<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

International Journal of Molecular Sciences published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Synthetic Route of 724710-02-5<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[801,131],"tags":[732],"class_list":["post-11796","post","type-post","status-publish","format-standard","hentry","category-724710-02-5","category-pyrazoles-derivatives","tag-m-w100-150"],"yoast_head":"\nReiberger, Robert's team published research in International Journal of Molecular Sciences in 22 | CAS: 724710-02-5 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Reiberger, Robert published the artcileSynthesis and In Vitro Evaluation of C-7 and C-8 Luteolin Derivatives as Influenza Endonuclease Inhibitors, Synthetic Route of 724710-02-5, the publication is International Journal of Molecular Sciences (2021), 22(14), 7735, database is CAplus and MEDLINE.\" \/>\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=11796\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Reiberger, Robert's team published research in International Journal of Molecular Sciences in 22 | CAS: 724710-02-5 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Reiberger, Robert published the artcileSynthesis and In Vitro Evaluation of C-7 and C-8 Luteolin Derivatives as Influenza Endonuclease Inhibitors, Synthetic Route of 724710-02-5, the publication is International Journal of Molecular Sciences (2021), 22(14), 7735, database is CAplus and MEDLINE.\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=11796\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-12-04T18:37:14+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\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11796\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11796\",\"name\":\"Reiberger, Robert's team published research in International Journal of Molecular Sciences in 22 | CAS: 724710-02-5 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-12-04T18:37:14+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Reiberger, Robert published the artcileSynthesis and In Vitro Evaluation of C-7 and C-8 Luteolin Derivatives as Influenza Endonuclease Inhibitors, Synthetic Route of 724710-02-5, the publication is International Journal of Molecular Sciences (2021), 22(14), 7735, database is CAplus and MEDLINE.\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11796#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=11796\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11796#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Reiberger, Robert’s team published research in International Journal of Molecular Sciences in 22 | CAS: 724710-02-5\"}]},{\"@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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