{"id":11215,"date":"2022-11-21T05:05:22","date_gmt":"2022-11-20T21:05:22","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11215"},"modified":"2022-11-21T05:05:22","modified_gmt":"2022-11-20T21:05:22","slug":"remya-chandrans-team-published-research-in-computational-and-structural-biotechnology-journal-in-19-cas-724710-02-5","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11215","title":{"rendered":"Remya, Chandran&#8217;s team published research in Computational and Structural Biotechnology Journal  in 19 | CAS: 724710-02-5"},"content":{"rendered":"<p>Remya, Chandran published the artcile<b><i>Neuroprotective derivatives of tacrine that target NMDA receptor and acetyl cholinesterase &#8211; Design, synthesis and biological evaluation<\/i><\/b>,  <a href=\"https:\/\/www.ambeed.com\/products\/724710-02-5.html\">Recommanded Product: (1H-Pyrazol-5-yl)boronic acid<\/a>,  the publication is  Computational and Structural Biotechnology Journal (2021), 4517-4537, database is CAplus and MEDLINE.<\/p>\n<p>An novel high affinity multi-target directed ligands (MTDLs) against AChE and NMDAR, with reduced hepatotoxicity, performed in-silico structure-based modifications on tacrine, chem. synthesis of the derivatives and in-vitro validation of their activities. Nineteen such derivatives <strong>I<\/strong> [R = H, methylcarbamoyl, hydrazinecarbonyl, ethoxycarbonyl; R<sup>1<\/sup> = 2-furanyl, 1-methylpyrazol-4-yl, 2-FC<sub>6<\/sub>H<sub>4<\/sub>, etc.] showed inhibition with IC<sub>50<\/sub> values in the range of 18.53 \u00b1 2.09 &#8211; 184.09 \u00b1 19.23 nM against AChE and 0.27 \u00b1 0.05 &#8211; 38.84 \u00b1 9.64\u03bcM against NMDAR. Some of the selected compounds protected rat primary cortical neurons from glutamate induced excitotoxicity. Two of the tacrine derived MTDLs, <strong>I<\/strong> [R = H, R<sup>1<\/sup> = 1-methylpyrazol-4-yl; R = H, R<sup>1<\/sup> = 2-FC<sub>6<\/sub>H<sub>4<\/sub>] exhibited in-vivo efficacy in rats by protecting against behavioral impairment induced by administration of the excitotoxic agent, monosodium glutamate. Addnl., several of these synthesized compounds also exhibited promising inhibitory activitiy against butyrylcholinesterase. MTDL-201 <strong>I<\/strong> [R = H, R<sup>1<\/sup> = 1-methylpyrazol-4-yl] was also devoid of hepatotoxicity in-vivo. Given the therapeutic potential of MTDLs in disease-modifying therapy, studies revealed several promising MTDLs among which <strong>I<\/strong> [R = H, R<sup>1<\/sup> = 1-methylpyrazol-4-yl] appeared to be a potential candidate for immediate preclin. evaluations.<\/p>\n<p>Computational and Structural Biotechnology Journal published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, <a href=\"https:\/\/www.ambeed.com\/products\/724710-02-5.html\">Recommanded Product: (1H-Pyrazol-5-yl)boronic acid<\/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>Computational and Structural Biotechnology Journal published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, <a href=\"https:\/\/www.ambeed.com\/products\/724710-02-5.html\">Recommanded Product: (1H-Pyrazol-5-yl)boronic acid<\/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":[732],"class_list":["post-11215","post","type-post","status-publish","format-standard","hentry","category-pyrazoles-derivatives","tag-m-w100-150"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - 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