{"id":12163,"date":"2023-02-03T04:14:56","date_gmt":"2023-02-02T20:14:56","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=12163"},"modified":"2023-02-03T04:14:56","modified_gmt":"2023-02-02T20:14:56","slug":"zhang-lei-et-al-published-their-research-in-journal-of-medicinal-chemistry-in-2014-cas-63725-52-0-2","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=12163","title":{"rendered":"Zhang, Lei et al. published their research in Journal of Medicinal Chemistry in 2014 | CAS: 63725-52-0"},"content":{"rendered":"<p>Discovery and Preclinical Characterization of 1-Methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]-pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator was written by Zhang, Lei;Balan, Gayatri;Barreiro, Gabriela;Boscoe, Brian P.;Chenard, Lois K.;Cianfrogna, Julie;Claffey, Michelle M.;Chen, Laigao;Coffman, Karen J.;Drozda, Susan E.;Dunetz, Joshua R.;Fonseca, Kari R.;Galatsis, Paul;Grimwood, Sarah;Lazzaro, John T.;Mancuso, Jessica Y.;Miller, Emily L.;Reese, Matthew R.;Rogers, Bruce N.;Sakurada, Isao;Skaddan, Marc;Smith, Deborah L.;Stepan, Antonia F.;Trapa, Patrick;Tuttle, Jamison B.;Verhoest, Patrick R.;Walker, Daniel P.;Wright, Ann S.;Zaleska, Margaret M.;Zasadny, Kenneth;Shaffer, Christopher L.. And the article was included in Journal of Medicinal Chemistry in 2014.<a href=\"https:\/\/www.ambeed.com\/products\/63725-52-0.html\">Electric Literature of C7H6ClN3<\/a> This article mentions the following:<\/p>\n<p>A novel series of pyrazolopyrazines is herein disclosed as mGluR5 neg. allosteric modulators (NAMs). Starting from a high-throughput screen (HTS) hit (1), a systematic structure-activity relationship (SAR) study was conducted with a specific focus on balancing pharmacol. potency with physicochem. and pharmacokinetic (PK) properties. This effort led to the discovery of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]-pyrazine (PF470, 14) as a highly potent, selective, and orally bioavailable mGluR5 NAM. Compound 14 demonstrated robust efficacy in a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-rendered Parkinsonian nonhuman primate model of l-DOPA-induced dyskinesia (PD-LID). However, the progression of 14 to the clinic was terminated because of a potentially mechanism-mediated finding consistent with a delayed-type immune-mediated type IV hypersensitivity in a 90-day NHP regulatory toxicol. study. In the experiment, the researchers used many compounds, for example, 6-Chloro-1-methylpyrazolo[5,4-b]pyridine (cas: 63725-52-0<a href=\"https:\/\/www.ambeed.com\/products\/63725-52-0.html\">Electric Literature of C7H6ClN3<\/a>).<\/p>\n<p>6-Chloro-1-methylpyrazolo[5,4-b]pyridine (cas: 63725-52-0) belongs to pyrazole derivatives. As is the case with imidazoles, the pyrazole ring offers many opportunities to create new multiring systems that incorporate this heterocycle. Pyrazole rings have been used as core components of several leading non-steroidal anti-inflammatory drugs (NSAIDs) and antihypertensive drugs. It has also been found to be useful as a bifunctional ligand for metal catalysis.<a href=\"https:\/\/www.ambeed.com\/products\/63725-52-0.html\">Electric Literature of C7H6ClN3<\/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>6-Chloro-1-methylpyrazolo[5,4-b]pyridine (cas: 63725-52-0) belongs to pyrazole derivatives. As is the case with imidazoles, the pyrazole ring offers many opportunities to create new multiring systems that incorporate this heterocycle. Pyrazole rings have been used as core components of several leading non-steroidal anti-inflammatory drugs (NSAIDs) and antihypertensive drugs. It has also been found to be useful as a bifunctional ligand for metal catalysis.<a href=\"https:\/\/www.ambeed.com\/products\/63725-52-0.html\">Electric Literature of C7H6ClN3<\/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-12163","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>Zhang, Lei et al. published their research in Journal of Medicinal Chemistry in 2014 | CAS: 63725-52-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Discovery and Preclinical Characterization of 1-Methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]-pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator was written by Zhang, Lei;Balan, Gayatri;Barreiro, Gabriela;Boscoe, Brian P.;Chenard, Lois K.;Cianfrogna, Julie;Claffey, Michelle M.;Chen, Laigao;Coffman, Karen J.;Drozda, Susan E.;Dunetz, Joshua R.;Fonseca, Kari R.;Galatsis, Paul;Grimwood, Sarah;Lazzaro, John T.;Mancuso, Jessica Y.;Miller, Emily L.;Reese, Matthew R.;Rogers, Bruce N.;Sakurada, Isao;Skaddan, Marc;Smith, Deborah L.;Stepan, Antonia F.;Trapa, Patrick;Tuttle, Jamison B.;Verhoest, Patrick R.;Walker, Daniel P.;Wright, Ann S.;Zaleska, Margaret M.;Zasadny, Kenneth;Shaffer, Christopher L.. And the article was included in Journal of Medicinal Chemistry in 2014.Electric Literature of C7H6ClN3 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=12163\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Zhang, Lei et al. published their research in Journal of Medicinal Chemistry in 2014 | CAS: 63725-52-0 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Discovery and Preclinical Characterization of 1-Methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]-pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator was written by Zhang, Lei;Balan, Gayatri;Barreiro, Gabriela;Boscoe, Brian P.;Chenard, Lois K.;Cianfrogna, Julie;Claffey, Michelle M.;Chen, Laigao;Coffman, Karen J.;Drozda, Susan E.;Dunetz, Joshua R.;Fonseca, Kari R.;Galatsis, Paul;Grimwood, Sarah;Lazzaro, John T.;Mancuso, Jessica Y.;Miller, Emily L.;Reese, Matthew R.;Rogers, Bruce N.;Sakurada, Isao;Skaddan, Marc;Smith, Deborah L.;Stepan, Antonia F.;Trapa, Patrick;Tuttle, Jamison B.;Verhoest, Patrick R.;Walker, Daniel P.;Wright, Ann S.;Zaleska, Margaret M.;Zasadny, Kenneth;Shaffer, Christopher L.. 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And the article was included in Journal of Medicinal Chemistry in 2014.Electric Literature of C7H6ClN3 This article mentions the following:","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=12163","og_locale":"en_US","og_type":"article","og_title":"Zhang, Lei et al. published their research in Journal of Medicinal Chemistry in 2014 | CAS: 63725-52-0 | pyrazoles-derivatives","og_description":"Discovery and Preclinical Characterization of 1-Methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]-pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator was written by Zhang, Lei;Balan, Gayatri;Barreiro, Gabriela;Boscoe, Brian P.;Chenard, Lois K.;Cianfrogna, Julie;Claffey, Michelle M.;Chen, Laigao;Coffman, Karen J.;Drozda, Susan E.;Dunetz, Joshua R.;Fonseca, Kari R.;Galatsis, Paul;Grimwood, Sarah;Lazzaro, John T.;Mancuso, Jessica Y.;Miller, Emily L.;Reese, Matthew R.;Rogers, Bruce N.;Sakurada, Isao;Skaddan, Marc;Smith, Deborah L.;Stepan, Antonia F.;Trapa, Patrick;Tuttle, Jamison B.;Verhoest, Patrick R.;Walker, Daniel P.;Wright, Ann S.;Zaleska, Margaret M.;Zasadny, Kenneth;Shaffer, Christopher L.. And the article was included in Journal of Medicinal Chemistry in 2014.Electric Literature of C7H6ClN3 This article mentions the following:","og_url":"https:\/\/www.pyrazoles-derivatives.com\/?p=12163","og_site_name":"pyrazoles-derivatives","article_published_time":"2023-02-02T20:14:56+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=12163","url":"https:\/\/www.pyrazoles-derivatives.com\/?p=12163","name":"Zhang, Lei et al. published their research in Journal of Medicinal Chemistry in 2014 | CAS: 63725-52-0 | pyrazoles-derivatives","isPartOf":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#website"},"datePublished":"2023-02-02T20:14:56+00:00","author":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1"},"description":"Discovery and Preclinical Characterization of 1-Methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]-pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator was written by Zhang, Lei;Balan, Gayatri;Barreiro, Gabriela;Boscoe, Brian P.;Chenard, Lois K.;Cianfrogna, Julie;Claffey, Michelle M.;Chen, Laigao;Coffman, Karen J.;Drozda, Susan E.;Dunetz, Joshua R.;Fonseca, Kari R.;Galatsis, Paul;Grimwood, Sarah;Lazzaro, John T.;Mancuso, Jessica Y.;Miller, Emily L.;Reese, Matthew R.;Rogers, Bruce N.;Sakurada, Isao;Skaddan, Marc;Smith, Deborah L.;Stepan, Antonia F.;Trapa, Patrick;Tuttle, Jamison B.;Verhoest, Patrick R.;Walker, Daniel P.;Wright, Ann S.;Zaleska, Margaret M.;Zasadny, Kenneth;Shaffer, Christopher L.. And the article was included in Journal of Medicinal Chemistry in 2014.Electric Literature of C7H6ClN3 This article mentions the following:","breadcrumb":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=12163#breadcrumb"},"inLanguage":"en-US","potentialAction":[{"@type":"ReadAction","target":["https:\/\/www.pyrazoles-derivatives.com\/?p=12163"]}]},{"@type":"BreadcrumbList","@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=12163#breadcrumb","itemListElement":[{"@type":"ListItem","position":1,"name":"\u9996\u9875","item":"https:\/\/www.pyrazoles-derivatives.com\/"},{"@type":"ListItem","position":2,"name":"Zhang, Lei et al. published their research in Journal of Medicinal Chemistry in 2014 | CAS: 63725-52-0"}]},{"@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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