{"id":11283,"date":"2022-11-22T04:56:43","date_gmt":"2022-11-21T20:56:43","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11283"},"modified":"2022-11-22T04:56:43","modified_gmt":"2022-11-21T20:56:43","slug":"schirok-hartmut-et-al-published-their-research-in-chemmedchem-in-2008-cas-49834-67-5","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11283","title":{"rendered":"Schirok, Hartmut et al. published their research in ChemMedChem in 2008 | CAS: 49834-67-5"},"content":{"rendered":"<p>Design and synthesis of potent and selective azaindole-based Rho kinase (ROCK) inhibitors was written by Schirok, Hartmut;Kast, Raimund;Figueroa-Perez, Santiago;Bennabi, Samir;Gnoth, Mark J.;Feurer, Achim;Heckroth, Heike;Thutewohl, Michael;Paulsen, Holger;Knorr, Andreas;Huetter, Joachim;Lobell, Mario;Muenter, Klaus;Geiss, Volker;Ehmke, Heimo;Lang, Dieter;Radtke, Martin;Mittendorf, Joachim;Stasch, Johannes-Peter. And the article was included in ChemMedChem in 2008.<a href=\"https:\/\/www.ambeed.com\/products\/49834-67-5.html\">Electric Literature of C6H5N3O<\/a> The following contents are mentioned in the article:<\/p>\n<p>Rho kinase plays a pivotal role in several cellular processes such as vasoregulation, making it a suitable target for the treatment of hypertension and related disorders. We discovered a compound class of Rho kinase (ROCK) inhibitors containing a 7-azaindole hinge-binding scaffold tethered to an aminopyrimidine core. Herein we describe the structure-activity relationships elucidated through biochem. and functional assays. The introduction of suitable substituents at the 3-position of the bicyclic moiety led to an increase in activity, which was required to design compounds with favorable pharmacokinetic profile. Azaindole <strong>I<\/strong> was identified as a highly selective and orally available ROCK inhibitor able to cause a sustained blood pressure reduction in vivo. This study involved multiple reactions and reactants, such as 1H-Pyrazolo[3,4-b]pyridin-4-ol (cas: 49834-67-5<a href=\"https:\/\/www.ambeed.com\/products\/49834-67-5.html\">Electric Literature of C6H5N3O<\/a>).<\/p>\n<p>1H-Pyrazolo[3,4-b]pyridin-4-ol (cas: 49834-67-5) belongs to pyrazole derivatives. Pyrazole has two ring nitrogen atoms in which N1 is pyrrolic and N2 is pyridine-like. The N1 nitrogen is not reactive but is deprotonated in the presence of a base-forming anion. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.<a href=\"https:\/\/www.ambeed.com\/products\/49834-67-5.html\">Electric Literature of C6H5N3O<\/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>1H-Pyrazolo[3,4-b]pyridin-4-ol (cas: 49834-67-5) belongs to pyrazole derivatives. Pyrazole has two ring nitrogen atoms in which N1 is pyrrolic and N2 is pyridine-like. The N1 nitrogen is not reactive but is deprotonated in the presence of a base-forming anion. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.<a href=\"https:\/\/www.ambeed.com\/products\/49834-67-5.html\">Electric Literature of C6H5N3O<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[793,131],"tags":[128],"class_list":["post-11283","post","type-post","status-publish","format-standard","hentry","category-49834-67-5","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>Schirok, Hartmut et al. published their research in ChemMedChem in 2008 | CAS: 49834-67-5 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Design and synthesis of potent and selective azaindole-based Rho kinase (ROCK) inhibitors was written by Schirok, Hartmut;Kast, Raimund;Figueroa-Perez, Santiago;Bennabi, Samir;Gnoth, Mark J.;Feurer, Achim;Heckroth, Heike;Thutewohl, Michael;Paulsen, Holger;Knorr, Andreas;Huetter, Joachim;Lobell, Mario;Muenter, Klaus;Geiss, Volker;Ehmke, Heimo;Lang, Dieter;Radtke, Martin;Mittendorf, Joachim;Stasch, Johannes-Peter. And the article was included in ChemMedChem in 2008.Electric Literature of C6H5N3O The following contents are mentioned in the article:\" \/>\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=11283\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Schirok, Hartmut et al. published their research in ChemMedChem in 2008 | CAS: 49834-67-5 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Design and synthesis of potent and selective azaindole-based Rho kinase (ROCK) inhibitors was written by Schirok, Hartmut;Kast, Raimund;Figueroa-Perez, Santiago;Bennabi, Samir;Gnoth, Mark J.;Feurer, Achim;Heckroth, Heike;Thutewohl, Michael;Paulsen, Holger;Knorr, Andreas;Huetter, Joachim;Lobell, Mario;Muenter, Klaus;Geiss, Volker;Ehmke, Heimo;Lang, Dieter;Radtke, Martin;Mittendorf, Joachim;Stasch, Johannes-Peter. 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And the article was included in ChemMedChem in 2008.Electric Literature of C6H5N3O The following contents are mentioned in the article:","breadcrumb":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=11283#breadcrumb"},"inLanguage":"en-US","potentialAction":[{"@type":"ReadAction","target":["https:\/\/www.pyrazoles-derivatives.com\/?p=11283"]}]},{"@type":"BreadcrumbList","@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=11283#breadcrumb","itemListElement":[{"@type":"ListItem","position":1,"name":"\u9996\u9875","item":"https:\/\/www.pyrazoles-derivatives.com\/"},{"@type":"ListItem","position":2,"name":"Schirok, Hartmut et al. published their research in ChemMedChem in 2008 | CAS: 49834-67-5"}]},{"@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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