{"id":11498,"date":"2022-11-28T04:26:49","date_gmt":"2022-11-27T20:26:49","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11498"},"modified":"2022-11-28T04:26:49","modified_gmt":"2022-11-27T20:26:49","slug":"jagtap-ajit-dhananjays-team-published-research-in-bioorganic-chemistry-in-95-cas-930-36-9","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11498","title":{"rendered":"Jagtap, Ajit Dhananjay&#8217;s team published research in Bioorganic Chemistry  in 95 | CAS: 930-36-9"},"content":{"rendered":"<p>Jagtap, Ajit Dhananjay published the artcile<b><i>4-Substituted 2-amino-3,4-dihydroquinazolines with a 3-hairpin turn side chain as novel inhibitors of BACE-1<\/i><\/b>,  <a href=\"https:\/\/www.ambeed.com\/products\/930-36-9.html\">Recommanded Product: 1-Methylpyrazole<\/a>,  the publication is  Bioorganic Chemistry (2020), 103135, database is CAplus and MEDLINE.<\/p>\n<p>Herein, the authors report the identification, design, and synthesis of a series of 4-substituted 2-amino-3,4-dihydroquinazolines <strong>I<\/strong> [R<sup>1<\/sup> = Me, CH:CH<sub>2<\/sub>, Bn, etc., R<sup>2<\/sup> = 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 <strong>II<\/strong> to the C4-position on the 3,4-dihydroquinazoline scaffold to facilitate interactions with the S<sub>1<\/sub>, S<sub>2<\/sub> and S<sub>1<\/sub>&#8216; subsites of BACE-1. Among these derivatives, two compounds exhibited potent BACE-1 inhibitory activity: 4-methyl-substituted derivative <strong>I<\/strong> [R<sup>1<\/sup> = Me, R<sup>2<\/sup> = (1-methyl-1H-pyrazol-4-yl)methyl] (BACE-1 CFA IC<sub>50<\/sub> = 0.38\u03bcM; BACE-1 WCA IC<sub>50<\/sub> = 0.14\u03bcM) and 4-cyclohexylmethyl-substituted derivative <strong>I<\/strong> [R<sup>1<\/sup> = cyclohexylmethyl, R<sup>2<\/sup> = (1-methyl-1H-pyrazol-4-yl)methyl] (BACE-1 CFA IC<sub>50<\/sub> = 0.49\u03bcM; BACE-1 WCA IC<sub>50<\/sub> = 0.14\u03bcM). The results suggest that the structural modifications maintain the hairpin turn topol. similar to that of compound <strong>II<\/strong> and provide an addnl. interaction with the S<sub>2<\/sub> subsite.<\/p>\n<p>Bioorganic Chemistry published new progress about 930-36-9. 930-36-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole, name is 1-Methylpyrazole, and the molecular formula is C4H6N2, <a href=\"https:\/\/www.ambeed.com\/products\/930-36-9.html\">Recommanded Product: 1-Methylpyrazole<\/a>.<\/p>\n<p>Referemce:<br \/><a href=\"https:\/\/en.wikipedia.org\/wiki\/Pyrazole\">https:\/\/en.wikipedia.org\/wiki\/Pyrazole<\/a>,<br \/><a href=\"Pyrazole - Wikipedia\">Pyrazoles &#8211; an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>Bioorganic Chemistry published new progress about 930-36-9. 930-36-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole, name is 1-Methylpyrazole, and the molecular formula is C4H6N2, <a href=\"https:\/\/www.ambeed.com\/products\/930-36-9.html\">Recommanded Product: 1-Methylpyrazole<\/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":[784],"class_list":["post-11498","post","type-post","status-publish","format-standard","hentry","category-930-36-9","category-pyrazoles-derivatives","tag-m-w50-100"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - 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