{"id":11937,"date":"2023-01-04T08:11:31","date_gmt":"2023-01-04T00:11:31","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11937"},"modified":"2023-01-04T08:11:31","modified_gmt":"2023-01-04T00:11:31","slug":"lunniss-c-et-al-published-their-research-in-bioorganic-medicinal-chemistry-letters-in-2010-cas-3528-58-3","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11937","title":{"rendered":"Lunniss, C. et al. published their research in Bioorganic &amp; Medicinal Chemistry Letters in 2010 | CAS: 3528-58-3"},"content":{"rendered":"<p>Addressing species specific metabolism and solubility issues in a quinoline series of oral PDE4 inhibitors was written by Lunniss, C.;Eldred, C.;Aston, N.;Craven, A.;Gohil, K.;Judkins, B.;Keeling, S.;Ranshaw, L.;Robinson, E.;Shipley, T.;Trivedi, N.. And the article was included in Bioorganic &amp; Medicinal Chemistry Letters in 2010.<a href=\"https:\/\/www.ambeed.com\/products\/3528-58-3.html\">Related Products of 3528-58-3<\/a> This article mentions the following:<\/p>\n<p>Species specific conversion of the lead PDE4 inhibitor 1 to the quinolone 3 was identified as the major route of metabolism in the cynomolgus monkey. Modification of the template to give the cinnoline 9 retained potency and selectivity, and greatly improved the pharmacokinetic profile in the cynomolgus monkey compared with 1. Addnl. SAR studies aimed at improving the solubility of 9 are also described. In the experiment, the researchers used many compounds, for example, 1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3<a href=\"https:\/\/www.ambeed.com\/products\/3528-58-3.html\">Related Products of 3528-58-3<\/a>).<\/p>\n<p>1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3) belongs to pyrazole derivatives. Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities.  The presence of both electronegative nitrogen atoms in the pyrazole ring reduces the electron density of the C3- and C5-positions leaving electron density of C4-position unaltered. Thus the C4-position is vulnerable to electrophilic attack. The C3 electrophilic-position may undergo deprotonation in the presence of a strong base leading to ring opening.<a href=\"https:\/\/www.ambeed.com\/products\/3528-58-3.html\">Related Products of 3528-58-3<\/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-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3) belongs to pyrazole derivatives. Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities.  The presence of both electronegative nitrogen atoms in the pyrazole ring reduces the electron density of the C3- and C5-positions leaving electron density of C4-position unaltered. Thus the C4-position is vulnerable to electrophilic attack. The C3 electrophilic-position may undergo deprotonation in the presence of a strong base leading to ring opening.<a href=\"https:\/\/www.ambeed.com\/products\/3528-58-3.html\">Related Products of 3528-58-3<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[131],"tags":[128],"class_list":["post-11937","post","type-post","status-publish","format-standard","hentry","category-pyrazoles-derivatives","tag-100-200"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Lunniss, C. et al. published their research in Bioorganic &amp; Medicinal Chemistry Letters in 2010 | CAS: 3528-58-3 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Addressing species specific metabolism and solubility issues in a quinoline series of oral PDE4 inhibitors was written by Lunniss, C.;Eldred, C.;Aston, N.;Craven, A.;Gohil, K.;Judkins, B.;Keeling, S.;Ranshaw, L.;Robinson, E.;Shipley, T.;Trivedi, N.. And the article was included in Bioorganic &amp; Medicinal Chemistry Letters in 2010.Related Products of 3528-58-3 This article mentions the following:\" \/>\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=11937\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Lunniss, C. et al. published their research in Bioorganic &amp; Medicinal Chemistry Letters in 2010 | CAS: 3528-58-3 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Addressing species specific metabolism and solubility issues in a quinoline series of oral PDE4 inhibitors was written by Lunniss, C.;Eldred, C.;Aston, N.;Craven, A.;Gohil, K.;Judkins, B.;Keeling, S.;Ranshaw, L.;Robinson, E.;Shipley, T.;Trivedi, N.. 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And the article was included in Bioorganic &amp; Medicinal Chemistry Letters in 2010.Related Products of 3528-58-3 This article mentions the following:","og_url":"https:\/\/www.pyrazoles-derivatives.com\/?p=11937","og_site_name":"pyrazoles-derivatives","article_published_time":"2023-01-04T00:11:31+00:00","author":"Jessica.F","twitter_card":"summary_large_image","twitter_misc":{"Written by":"Jessica.F","Est. reading time":"1 minute"},"schema":{"@context":"https:\/\/schema.org","@graph":[{"@type":"WebPage","@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=11937","url":"https:\/\/www.pyrazoles-derivatives.com\/?p=11937","name":"Lunniss, C. et al. published their research in Bioorganic &amp; Medicinal Chemistry Letters in 2010 | CAS: 3528-58-3 | pyrazoles-derivatives","isPartOf":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#website"},"datePublished":"2023-01-04T00:11:31+00:00","author":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1"},"description":"Addressing species specific metabolism and solubility issues in a quinoline series of oral PDE4 inhibitors was written by Lunniss, C.;Eldred, C.;Aston, N.;Craven, A.;Gohil, K.;Judkins, B.;Keeling, S.;Ranshaw, L.;Robinson, E.;Shipley, T.;Trivedi, N.. And the article was included in Bioorganic &amp; Medicinal Chemistry Letters in 2010.Related Products of 3528-58-3 This article mentions the following:","breadcrumb":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=11937#breadcrumb"},"inLanguage":"en-US","potentialAction":[{"@type":"ReadAction","target":["https:\/\/www.pyrazoles-derivatives.com\/?p=11937"]}]},{"@type":"BreadcrumbList","@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=11937#breadcrumb","itemListElement":[{"@type":"ListItem","position":1,"name":"\u9996\u9875","item":"https:\/\/www.pyrazoles-derivatives.com\/"},{"@type":"ListItem","position":2,"name":"Lunniss, C. et al. published their research in Bioorganic &amp; Medicinal Chemistry Letters in 2010 | CAS: 3528-58-3"}]},{"@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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