{"id":11994,"date":"2023-01-05T03:44:33","date_gmt":"2023-01-04T19:44:33","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11994"},"modified":"2023-01-05T03:44:33","modified_gmt":"2023-01-04T19:44:33","slug":"le-thuy-g-et-al-published-their-research-in-journal-of-medicinal-chemistry-in-2018-cas-55361-49-4","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11994","title":{"rendered":"Le, Thuy G. et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 55361-49-4"},"content":{"rendered":"<p>Optimization of Novel 1-Methyl-1H-Pyrazole-5-carboxamides Leads to High Potency Larval Development Inhibitors of the Barber&#8217;s Pole Worm was written by Le, Thuy G.;Kundu, Abhijit;Ghoshal, Atanu;Nguyen, Nghi H.;Preston, Sarah;Jiao, Yaqing;Ruan, Banfeng;Xue, Lian;Huang, Fei;Keiser, Jennifer;Hofmann, Andreas;Chang, Bill C. H.;Garcia-Bustos, Jose;Jabbar, Abdul;Wells, Timothy N. C.;Palmer, Michael J.;Gasser, Robin B.;Baell, Jonathan B.. And the article was included in Journal of Medicinal Chemistry in 2018.<a href=\"https:\/\/www.ambeed.com\/products\/55361-49-4.html\">Synthetic Route of C5H9N3<\/a> This article mentions the following:<\/p>\n<p>A phenotypic screen of a diverse library of small mols. for inhibition of the development of larvae of the parasitic nematode Haemonchus contortus led to the identification of a 1-methyl-1H-pyrazole-5-carboxamide derivative with an IC<sub>50<\/sub> of 0.29 \u03bcM. Medicinal chem. optimization targeted modifications on the left-hand side (LHS), middle section, and right-hand side (RHS) of the scaffold to elucidate the structure-activity relation (SAR). Strong SAR allowed for the iterative and directed assembly of a focus set of 64 analogs, from which compound 60 was identified as the most potent compound, inhibiting the development of the fourth larval (L4) stage with an IC<sub>50<\/sub> of 0.01 \u03bcM. In contrast, only 18% inhibition of the mammary epithelial cell line MCF10A viability was observed, even at concentrations as high as 50 \u03bcM. In the experiment, the researchers used many compounds, for example, 1-Ethyl-1H-pyrazol-3-amine (cas: 55361-49-4<a href=\"https:\/\/www.ambeed.com\/products\/55361-49-4.html\">Synthetic Route of C5H9N3<\/a>).<\/p>\n<p>1-Ethyl-1H-pyrazol-3-amine (cas: 55361-49-4) belongs to pyrazole derivatives. The 1H-pyrazole provides an excellent means by which to provide the requisite hydrogen bond acceptor\u2013donor motifs, whether as a monocyclic ring or as a fused indazole ring. Pyrazole the presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. <a href=\"https:\/\/www.ambeed.com\/products\/55361-49-4.html\">Synthetic Route of C5H9N3<\/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-3-amine (cas: 55361-49-4) belongs to pyrazole derivatives. The 1H-pyrazole provides an excellent means by which to provide the requisite hydrogen bond acceptor\u2013donor motifs, whether as a monocyclic ring or as a fused indazole ring. Pyrazole the presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. <a href=\"https:\/\/www.ambeed.com\/products\/55361-49-4.html\">Synthetic Route of C5H9N3<\/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-11994","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>Le, Thuy G. et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 55361-49-4 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Optimization of Novel 1-Methyl-1H-Pyrazole-5-carboxamides Leads to High Potency Larval Development Inhibitors of the Barber&#039;s Pole Worm was written by Le, Thuy G.;Kundu, Abhijit;Ghoshal, Atanu;Nguyen, Nghi H.;Preston, Sarah;Jiao, Yaqing;Ruan, Banfeng;Xue, Lian;Huang, Fei;Keiser, Jennifer;Hofmann, Andreas;Chang, Bill C. H.;Garcia-Bustos, Jose;Jabbar, Abdul;Wells, Timothy N. C.;Palmer, Michael J.;Gasser, Robin B.;Baell, Jonathan B.. And the article was included in Journal of Medicinal Chemistry in 2018.Synthetic Route of C5H9N3 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=11994\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Le, Thuy G. et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 55361-49-4 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Optimization of Novel 1-Methyl-1H-Pyrazole-5-carboxamides Leads to High Potency Larval Development Inhibitors of the Barber&#039;s Pole Worm was written by Le, Thuy G.;Kundu, Abhijit;Ghoshal, Atanu;Nguyen, Nghi H.;Preston, Sarah;Jiao, Yaqing;Ruan, Banfeng;Xue, Lian;Huang, Fei;Keiser, Jennifer;Hofmann, Andreas;Chang, Bill C. H.;Garcia-Bustos, Jose;Jabbar, Abdul;Wells, Timothy N. C.;Palmer, Michael J.;Gasser, Robin B.;Baell, Jonathan B.. And the article was included in Journal of Medicinal Chemistry in 2018.Synthetic Route of C5H9N3 This article mentions the following:\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=11994\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2023-01-04T19:44:33+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=11994\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11994\",\"name\":\"Le, Thuy G. et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 55361-49-4 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2023-01-04T19:44:33+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Optimization of Novel 1-Methyl-1H-Pyrazole-5-carboxamides Leads to High Potency Larval Development Inhibitors of the Barber's Pole Worm was written by Le, Thuy G.;Kundu, Abhijit;Ghoshal, Atanu;Nguyen, Nghi H.;Preston, Sarah;Jiao, Yaqing;Ruan, Banfeng;Xue, Lian;Huang, Fei;Keiser, Jennifer;Hofmann, Andreas;Chang, Bill C. 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H.;Garcia-Bustos, Jose;Jabbar, Abdul;Wells, Timothy N. C.;Palmer, Michael J.;Gasser, Robin B.;Baell, Jonathan B.. And the article was included in Journal of Medicinal Chemistry in 2018.Synthetic Route of C5H9N3 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=11994","og_locale":"en_US","og_type":"article","og_title":"Le, Thuy G. et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 55361-49-4 | pyrazoles-derivatives","og_description":"Optimization of Novel 1-Methyl-1H-Pyrazole-5-carboxamides Leads to High Potency Larval Development Inhibitors of the Barber's Pole Worm was written by Le, Thuy G.;Kundu, Abhijit;Ghoshal, Atanu;Nguyen, Nghi H.;Preston, Sarah;Jiao, Yaqing;Ruan, Banfeng;Xue, Lian;Huang, Fei;Keiser, Jennifer;Hofmann, Andreas;Chang, Bill C. 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