{"id":10366,"date":"2022-10-20T04:13:53","date_gmt":"2022-10-19T20:13:53","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10366"},"modified":"2022-10-20T04:13:53","modified_gmt":"2022-10-19T20:13:53","slug":"jagtap-ajit-dhananjays-team-published-research-in-bioorganic-chemistry-in-2020-cas-930-36-9","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10366","title":{"rendered":"Jagtap, Ajit Dhananjay’s team published research in Bioorganic Chemistry in 2020 | CAS: 930-36-9"},"content":{"rendered":"

Jagtap, Ajit Dhananjay; Kondekar, Nagendra B.; Hung, Pei-Yun; Hsieh, Chen-En; Yang, Chia-Ron; Chen, Grace Shiahuy; Chern, Ji-Wang published an article on January 31 ,2020. The article was titled \u300a4-Substituted 2-amino-3,4-dihydroquinazolines with a 3-hairpin turn side chain as novel inhibitors of BACE-1\u300b, and you may find the article in Bioorganic Chemistry.Product Details of 930-36-9<\/a> The information in the text is summarized as follows:<\/p>\n

Herein, the authors report the identification, design, and synthesis of a series of 4-substituted 2-amino-3,4-dihydroquinazolines I [R1 = Me, CH:CH2, Bn, etc., R2 = Me, cyclopropyl, (1-methyl-1H-pyrazol-4-yl)methyl] with hairpin turn side chains as novel inhibitors of BACE-1. The dihydroquinazoline derivatives were rationally designed by modifying the amide group and relocating the \u03b1-hydrophobic substituent on the hairpin turn side chain of lead compound II to the C4-position on the 3,4-dihydroquinazoline scaffold to facilitate interactions with the S1, S2 and S1′ subsites of BACE-1. Among these derivatives, two compounds exhibited potent BACE-1 inhibitory activity: 4-methyl-substituted derivative I [R1 = Me, R2 = (1-methyl-1H-pyrazol-4-yl)methyl] (BACE-1 CFA IC50 = 0.38\u03bcM; BACE-1 WCA IC50 = 0.14\u03bcM) and 4-cyclohexylmethyl-substituted derivative I [R1 = cyclohexylmethyl, R2 = (1-methyl-1H-pyrazol-4-yl)methyl] (BACE-1 CFA IC50 = 0.49\u03bcM; BACE-1 WCA IC50 = 0.14\u03bcM). The results suggest that the structural modifications maintain the hairpin turn topol. similar to that of compound II and provide an addnl. interaction with the S2 subsite. The results came from multiple reactions, including the reaction of 1-Methylpyrazole(cas: 930-36-9Product Details of 930-36-9<\/a>)<\/p>\n

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Product Details of 930-36-9<\/a><\/p>\n

Referemce:
Pyrazole – Wikipedia<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Product Details of 930-36-9<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[245,131],"tags":[743],"class_list":["post-10366","post","type-post","status-publish","format-standard","hentry","category-930-36-9","category-pyrazoles-derivatives","tag-0-100"],"yoast_head":"\nJagtap, Ajit Dhananjay's team published research in Bioorganic Chemistry in 2020 | CAS: 930-36-9 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Jagtap, Ajit Dhananjay; Kondekar, Nagendra B.; Hung, Pei-Yun; Hsieh, Chen-En; Yang, Chia-Ron; Chen, Grace Shiahuy; Chern, Ji-Wang published an article on January 31 ,2020. The article was titled \u300a4-Substituted 2-amino-3,4-dihydroquinazolines with a 3-hairpin turn side chain as novel inhibitors of BACE-1\u300b, and you may find the article in Bioorganic Chemistry.Product Details of 930-36-9 The information in the text is summarized as follows:\" \/>\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=10366\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Jagtap, Ajit Dhananjay's team published research in Bioorganic Chemistry in 2020 | CAS: 930-36-9 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Jagtap, Ajit Dhananjay; Kondekar, Nagendra B.; Hung, Pei-Yun; Hsieh, Chen-En; Yang, Chia-Ron; Chen, Grace Shiahuy; Chern, Ji-Wang published an article on January 31 ,2020. The article was titled \u300a4-Substituted 2-amino-3,4-dihydroquinazolines with a 3-hairpin turn side chain as novel inhibitors of BACE-1\u300b, and you may find the article in Bioorganic Chemistry.Product Details of 930-36-9 The information in the text is summarized as follows:\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=10366\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-10-19T20:13:53+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=10366\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10366\",\"name\":\"Jagtap, Ajit Dhananjay's team published research in Bioorganic Chemistry in 2020 | CAS: 930-36-9 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-10-19T20:13:53+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Jagtap, Ajit Dhananjay; Kondekar, Nagendra B.; Hung, Pei-Yun; Hsieh, Chen-En; Yang, Chia-Ron; Chen, Grace Shiahuy; Chern, Ji-Wang published an article on January 31 ,2020. The article was titled \u300a4-Substituted 2-amino-3,4-dihydroquinazolines with a 3-hairpin turn side chain as novel inhibitors of BACE-1\u300b, and you may find the article in Bioorganic Chemistry.Product Details of 930-36-9 The information in the text is summarized as follows:\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10366#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=10366\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=10366#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Jagtap, Ajit Dhananjay’s team published research in Bioorganic Chemistry in 2020 | CAS: 930-36-9\"}]},{\"@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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