{"id":9709,"date":"2022-04-19T04:46:24","date_gmt":"2022-04-18T20:46:24","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=9709"},"modified":"2022-04-19T04:46:24","modified_gmt":"2022-04-18T20:46:24","slug":"interesting-scientific-research-on-1300746-79-5","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=9709","title":{"rendered":"Interesting scientific research on 1300746-79-5"},"content":{"rendered":"<p>Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 1300746-79-5, is researched, SMILESS is F[C-](F)([Cu+]1[N]2=C3C4=[N]1C=CC=C4C=CC3=CC=C2)F, Molecular C13H8CuF3N2Journal, Article, European Journal of Medicinal Chemistry called Novel donepezil-like N-benzylpyridinium salt derivatives as AChE inhibitors and their corresponding dihydropyridine &#8220;&#8221;bio-oxidizable&#8221;&#8221; prodrugs: Synthesis, biological evaluation and structure-activity relationship, Author is Azzouz, Rabah; Peauger, Ludovic; Gembus, Vincent; Tintas, Mihaela-Liliana; Sopkova-de Oliveira Santos, Jana; Papamicael, Cyril; Levacher, Vincent, the main research direction is benzylpyridinium salt dihydropyridine preparation antialzheimer mol docking; AChEIs; Alzheimer; Donepezil analogues; \u201cBio-oxidizable\u201d prodrug.<a href=\"https:\/\/www.ambeed.com\/products\/1300746-79-5.html\">Category: pyrazoles-derivatives<\/a>.<\/p>\n<p>A total of fifty one N-benzylpyridinium quaternary donepezil analogs B1-3 I [R = Ph, 2,3-dihydro-1,3-benzoxazol-2-yl, cyclohexyl, etc.; R1 = H, F, OH, OCH3; R2 = H, OCH3; R1, R2 = -OCH2O-; EWG = H, CN, CF3, C(O)NH2, etc.; X = Br, I; n = 0, 1, 2] and twenty two prodrugs A1-3 II was synthesized and evaluated for their inhibitory activities against hAChE and eqBuChE. While most prodrugs A1-3 were demonstrated to be inactive against AChE (IC50 >10 \u03bcM), a large number of the corresponding N-benzylpyridinium salt B1-3 exhibited appealing three-to-one-digit nanomolar hAChE inhibitory activities and even reaching subnanomolar activity (IC50 = 0.36 nM). In addition, in silico docking studies were conducted for several compounds to explain the more relevant in vitro results. Lastly, the influence of the two stereogenic centers in prodrugs A was also evaluated, highlighting not only marked differences in residual AChE inhibitory activity of the four separated isomers of prodrug II [R = 3-chlorophenyl; R1 = H, F, OH, OCH3; R2 = OCH3; EWG = C(O)NH2;n = 1] (IC50 ranging from 173 nM to 10 \u03bcM) but also significant variations of the oxidation rate between two separated diastereoisomers of prodrug II [R = phenyl; R1 = R2 = OCH3; EWG = C(O)CH3; n = 2]. This work provides useful information in the search of a preclin. candidate to conduct further development of this attractive &#8220;&#8221;bio-oxidizable&#8221;&#8221; prodrug strategy.<\/p>\n<p>Different reactions of this compound((1,10-Phenanthroline)(trifluoromethyl)copper(I))<a href=\"https:\/\/www.ambeed.com\/products\/1300746-79-5.html\">Category: pyrazoles-derivatives<\/a> require different conditions, so the reaction conditions are very important.<\/p>\n<p>Reference:<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>Different reactions of this compound((1,10-Phenanthroline)(trifluoromethyl)copper(I))<a href=\"https:\/\/www.ambeed.com\/products\/1300746-79-5.html\">Category: pyrazoles-derivatives<\/a> require different conditions, so the reaction conditions are very important.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[726,131],"tags":[167],"class_list":["post-9709","post","type-post","status-publish","format-standard","hentry","category-1300746-79-5","category-pyrazoles-derivatives","tag-m-w300-400"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Interesting scientific research on 1300746-79-5 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 1300746-79-5, is researched, SMILESS is F[C-](F)([Cu+]1[N]2=C3C4=[N]1C=CC=C4C=CC3=CC=C2)F, Molecular C13H8CuF3N2Journal, Article, European Journal of Medicinal Chemistry called Novel donepezil-like N-benzylpyridinium salt derivatives as AChE inhibitors and their corresponding dihydropyridine &quot;&quot;bio-oxidizable&quot;&quot; prodrugs: Synthesis, biological evaluation and structure-activity relationship, Author is Azzouz, Rabah; Peauger, Ludovic; Gembus, Vincent; Tintas, Mihaela-Liliana; Sopkova-de Oliveira Santos, Jana; Papamicael, Cyril; Levacher, Vincent, the main research direction is benzylpyridinium salt dihydropyridine preparation antialzheimer mol docking; AChEIs; Alzheimer; Donepezil analogues; \u201cBio-oxidizable\u201d prodrug.Category: pyrazoles-derivatives.\" \/>\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=9709\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Interesting scientific research on 1300746-79-5 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 1300746-79-5, is researched, SMILESS is F[C-](F)([Cu+]1[N]2=C3C4=[N]1C=CC=C4C=CC3=CC=C2)F, Molecular C13H8CuF3N2Journal, Article, European Journal of Medicinal Chemistry called Novel donepezil-like N-benzylpyridinium salt derivatives as AChE inhibitors and their corresponding dihydropyridine &quot;&quot;bio-oxidizable&quot;&quot; prodrugs: Synthesis, biological evaluation and structure-activity relationship, Author is Azzouz, Rabah; Peauger, Ludovic; Gembus, Vincent; Tintas, Mihaela-Liliana; Sopkova-de Oliveira Santos, Jana; Papamicael, Cyril; Levacher, Vincent, the main research direction is benzylpyridinium salt dihydropyridine preparation antialzheimer mol docking; AChEIs; Alzheimer; Donepezil analogues; \u201cBio-oxidizable\u201d prodrug.Category: pyrazoles-derivatives.\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=9709\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-04-18T20:46:24+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=9709\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=9709\",\"name\":\"Interesting scientific research on 1300746-79-5 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-04-18T20:46:24+00:00\",\"author\":{\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. 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