{"id":11266,"date":"2022-11-22T04:55:21","date_gmt":"2022-11-21T20:55:21","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11266"},"modified":"2022-11-22T04:55:21","modified_gmt":"2022-11-21T20:55:21","slug":"aghazadeh-tabrizi-mojgan-et-al-published-their-research-in-journal-of-medicinal-chemistry-in-2018-cas-17355-75-8","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11266","title":{"rendered":"Aghazadeh-Tabrizi, Mojgan et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 17355-75-8"},"content":{"rendered":"<p>Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors was written by Aghazadeh-Tabrizi, Mojgan;Baraldi, Pier Giovanni;Baraldi, Stefania;Ruggiero, Emanuela;De Stefano, Lucia;Rizzolio, Flavio;Di Cesare Mannelli, Lorenzo;Ghelardini, Carla;Chicca, Andrea;Lapillo, Margherita;Gertsch, Jurg;Manera, Clementina;Macchia, Marco;Martinelli, Adriano;Granchi, Carlotta;Minutolo, Filippo;Tuccinardi, Tiziano. And the article was included in Journal of Medicinal Chemistry in 2018.<a href=\"https:\/\/www.ambeed.com\/products\/17355-75-8.html\">COA of Formula: C18H16N2O2<\/a> The following contents are mentioned in the article:<\/p>\n<p>Monoacylglycerol lipase (MAGL) is a serine hydrolase that plays an important role in the degradation of the endocannabinoid neurotransmitter 2-arachidonoylglycerol, which is implicated in many physiol. processes. Beyond the possible utilization of MAGL inhibitors as anti-inflammatory, antinociceptive, and anticancer agents, their application has encountered obstacles due to the unwanted effects caused by the irreversible inhibition of this enzyme. The possible application of reversible MAGL inhibitors has only recently been explored, mainly due to the deficiency of known compounds possessing efficient reversible inhibitory activities. The authors report a new series of reversible MAGL inhibitors. Among them, compound 26 ((4-benzylpiperidin-1-yl)(5-(4-hydroxyphenyl)-1-(3-methylbenzyl)-1H-pyrazol-3-yl)methanone) showed to be a potent MAGL inhibitor (IC<sub>50<\/sub> = 0.51 \u03bcM, K<sub>i<\/sub> = 412 nM) with a good selectivity vs. fatty acid amide hydrolase (FAAH), \u03b1\/\u03b2-hydrolase domain-containing 6 (ABHD6), and 12 (ABHD12). Interestingly, this compound also possesses antiproliferative activities against two different cancer cell lines and relieves the neuropathic hypersensitivity induced in vivo by oxaliplatin. This study involved multiple reactions and reactants, such as Ethyl 1,5-diphenyl-1H-pyrazole-3-carboxylate (cas: 17355-75-8<a href=\"https:\/\/www.ambeed.com\/products\/17355-75-8.html\">COA of Formula: C18H16N2O2<\/a>).<\/p>\n<p>Ethyl 1,5-diphenyl-1H-pyrazole-3-carboxylate (cas: 17355-75-8) belongs to pyrazole derivatives. Pyrazoles, a five-membered heterocycle containing two adjacent nitrogen atoms, are the core structures found in a number of molecules that possess a wide range of pharmaceutical and agricultural 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\/17355-75-8.html\">COA of Formula: C18H16N2O2<\/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>Ethyl 1,5-diphenyl-1H-pyrazole-3-carboxylate (cas: 17355-75-8) belongs to pyrazole derivatives. Pyrazoles, a five-membered heterocycle containing two adjacent nitrogen atoms, are the core structures found in a number of molecules that possess a wide range of pharmaceutical and agricultural 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\/17355-75-8.html\">COA of Formula: C18H16N2O2<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[786,131],"tags":[129],"class_list":["post-11266","post","type-post","status-publish","format-standard","hentry","category-17355-75-8","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>Aghazadeh-Tabrizi, Mojgan et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 17355-75-8 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors was written by Aghazadeh-Tabrizi, Mojgan;Baraldi, Pier Giovanni;Baraldi, Stefania;Ruggiero, Emanuela;De Stefano, Lucia;Rizzolio, Flavio;Di Cesare Mannelli, Lorenzo;Ghelardini, Carla;Chicca, Andrea;Lapillo, Margherita;Gertsch, Jurg;Manera, Clementina;Macchia, Marco;Martinelli, Adriano;Granchi, Carlotta;Minutolo, Filippo;Tuccinardi, Tiziano. And the article was included in Journal of Medicinal Chemistry in 2018.COA of Formula: C18H16N2O2 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=11266\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Aghazadeh-Tabrizi, Mojgan et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 17355-75-8 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors was written by Aghazadeh-Tabrizi, Mojgan;Baraldi, Pier Giovanni;Baraldi, Stefania;Ruggiero, Emanuela;De Stefano, Lucia;Rizzolio, Flavio;Di Cesare Mannelli, Lorenzo;Ghelardini, Carla;Chicca, Andrea;Lapillo, Margherita;Gertsch, Jurg;Manera, Clementina;Macchia, Marco;Martinelli, Adriano;Granchi, Carlotta;Minutolo, Filippo;Tuccinardi, Tiziano. And the article was included in Journal of Medicinal Chemistry in 2018.COA of Formula: C18H16N2O2 The following contents are mentioned in the article:\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=11266\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-11-21T20:55:21+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=\"2 minutes\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\/\/schema.org\",\"@graph\":[{\"@type\":\"WebPage\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11266\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11266\",\"name\":\"Aghazadeh-Tabrizi, Mojgan et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 17355-75-8 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-11-21T20:55:21+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors was written by Aghazadeh-Tabrizi, Mojgan;Baraldi, Pier Giovanni;Baraldi, Stefania;Ruggiero, Emanuela;De Stefano, Lucia;Rizzolio, Flavio;Di Cesare Mannelli, Lorenzo;Ghelardini, Carla;Chicca, Andrea;Lapillo, Margherita;Gertsch, Jurg;Manera, Clementina;Macchia, Marco;Martinelli, Adriano;Granchi, Carlotta;Minutolo, Filippo;Tuccinardi, Tiziano. And the article was included in Journal of Medicinal Chemistry in 2018.COA of Formula: C18H16N2O2 The following contents are mentioned in the article:\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11266#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=11266\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11266#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Aghazadeh-Tabrizi, Mojgan et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 17355-75-8\"}]},{\"@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. Pyrazole derivatives play an important role in antitumor agents.\",\"potentialAction\":[{\"@type\":\"SearchAction\",\"target\":{\"@type\":\"EntryPoint\",\"urlTemplate\":\"https:\/\/www.pyrazoles-derivatives.com\/?s={search_term_string}\"},\"query-input\":{\"@type\":\"PropertyValueSpecification\",\"valueRequired\":true,\"valueName\":\"search_term_string\"}}],\"inLanguage\":\"en-US\"},{\"@type\":\"Person\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\",\"name\":\"Jessica.F\",\"image\":{\"@type\":\"ImageObject\",\"inLanguage\":\"en-US\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/image\/\",\"url\":\"https:\/\/en.cravatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g\",\"contentUrl\":\"https:\/\/en.cravatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g\",\"caption\":\"Jessica.F\"}}]}<\/script>\n<!-- \/ Yoast SEO plugin. -->","yoast_head_json":{"title":"Aghazadeh-Tabrizi, Mojgan et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 17355-75-8 | pyrazoles-derivatives","description":"Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors was written by Aghazadeh-Tabrizi, Mojgan;Baraldi, Pier Giovanni;Baraldi, Stefania;Ruggiero, Emanuela;De Stefano, Lucia;Rizzolio, Flavio;Di Cesare Mannelli, Lorenzo;Ghelardini, Carla;Chicca, Andrea;Lapillo, Margherita;Gertsch, Jurg;Manera, Clementina;Macchia, Marco;Martinelli, Adriano;Granchi, Carlotta;Minutolo, Filippo;Tuccinardi, Tiziano. And the article was included in Journal of Medicinal Chemistry in 2018.COA of Formula: C18H16N2O2 The following contents are mentioned in the article:","robots":{"index":"index","follow":"follow","max-snippet":"max-snippet:-1","max-image-preview":"max-image-preview:large","max-video-preview":"max-video-preview:-1"},"canonical":"https:\/\/www.pyrazoles-derivatives.com\/?p=11266","og_locale":"en_US","og_type":"article","og_title":"Aghazadeh-Tabrizi, Mojgan et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 17355-75-8 | pyrazoles-derivatives","og_description":"Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors was written by Aghazadeh-Tabrizi, Mojgan;Baraldi, Pier Giovanni;Baraldi, Stefania;Ruggiero, Emanuela;De Stefano, Lucia;Rizzolio, Flavio;Di Cesare Mannelli, Lorenzo;Ghelardini, Carla;Chicca, Andrea;Lapillo, Margherita;Gertsch, Jurg;Manera, Clementina;Macchia, Marco;Martinelli, Adriano;Granchi, Carlotta;Minutolo, Filippo;Tuccinardi, Tiziano. And the article was included in Journal of Medicinal Chemistry in 2018.COA of Formula: C18H16N2O2 The following contents are mentioned in the article:","og_url":"https:\/\/www.pyrazoles-derivatives.com\/?p=11266","og_site_name":"pyrazoles-derivatives","article_published_time":"2022-11-21T20:55:21+00:00","author":"Jessica.F","twitter_card":"summary_large_image","twitter_misc":{"Written by":"Jessica.F","Est. reading time":"2 minutes"},"schema":{"@context":"https:\/\/schema.org","@graph":[{"@type":"WebPage","@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=11266","url":"https:\/\/www.pyrazoles-derivatives.com\/?p=11266","name":"Aghazadeh-Tabrizi, Mojgan et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 17355-75-8 | pyrazoles-derivatives","isPartOf":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#website"},"datePublished":"2022-11-21T20:55:21+00:00","author":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1"},"description":"Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors was written by Aghazadeh-Tabrizi, Mojgan;Baraldi, Pier Giovanni;Baraldi, Stefania;Ruggiero, Emanuela;De Stefano, Lucia;Rizzolio, Flavio;Di Cesare Mannelli, Lorenzo;Ghelardini, Carla;Chicca, Andrea;Lapillo, Margherita;Gertsch, Jurg;Manera, Clementina;Macchia, Marco;Martinelli, Adriano;Granchi, Carlotta;Minutolo, Filippo;Tuccinardi, Tiziano. And the article was included in Journal of Medicinal Chemistry in 2018.COA of Formula: C18H16N2O2 The following contents are mentioned in the article:","breadcrumb":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=11266#breadcrumb"},"inLanguage":"en-US","potentialAction":[{"@type":"ReadAction","target":["https:\/\/www.pyrazoles-derivatives.com\/?p=11266"]}]},{"@type":"BreadcrumbList","@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=11266#breadcrumb","itemListElement":[{"@type":"ListItem","position":1,"name":"\u9996\u9875","item":"https:\/\/www.pyrazoles-derivatives.com\/"},{"@type":"ListItem","position":2,"name":"Aghazadeh-Tabrizi, Mojgan et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 17355-75-8"}]},{"@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. Pyrazole derivatives play an important role in antitumor agents.","potentialAction":[{"@type":"SearchAction","target":{"@type":"EntryPoint","urlTemplate":"https:\/\/www.pyrazoles-derivatives.com\/?s={search_term_string}"},"query-input":{"@type":"PropertyValueSpecification","valueRequired":true,"valueName":"search_term_string"}}],"inLanguage":"en-US"},{"@type":"Person","@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1","name":"Jessica.F","image":{"@type":"ImageObject","inLanguage":"en-US","@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/image\/","url":"https:\/\/en.cravatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g","contentUrl":"https:\/\/en.cravatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g","caption":"Jessica.F"}}]}},"_links":{"self":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/posts\/11266","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/users\/8"}],"replies":[{"embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=11266"}],"version-history":[{"count":0,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/posts\/11266\/revisions"}],"wp:attachment":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=11266"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=11266"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=11266"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}