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Search results for: quinazolines

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for: quinazolines</h1> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">2</span> Synthesis of New 2-(Methylthio) Benzo[g]-[1,2,4] Triazolo [1,5a] Quinazolines </h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Rashad%20A.%20Al-Salahi">Rashad A. Al-Salahi</a>, <a href="https://publications.waset.org/abstracts/search?q=Mohamed%20S.%20Marzouk"> Mohamed S. Marzouk</a> </p> <p class="card-text"><strong>Abstract:</strong></p> Aiming to the synthesis of bioactive triazoloquinazolines, a new series of 2-(methylthio)benzo [g]-[1,2,4] triazolo [1,5-a] quinazolin-5(4H)-ones was synthesized from 2-(methylthio)benzo [g]-[1,2,4] triazolo [1,5-a] quinazolin-5(4H)-one. All synthesized derivatives based on N-alkylation and chlorination of the parent compound and its salfonyl derivative. The success of the reactions was proved by NMR, IR, and HREI-MS analyses for all products. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=triazoloquinazoline" title="triazoloquinazoline">triazoloquinazoline</a>, <a href="https://publications.waset.org/abstracts/search?q=alkylation" title=" alkylation"> alkylation</a>, <a href="https://publications.waset.org/abstracts/search?q=thionation" title=" thionation"> thionation</a>, <a href="https://publications.waset.org/abstracts/search?q=quinazolin" title=" quinazolin"> quinazolin</a> </p> <a href="https://publications.waset.org/abstracts/21894/synthesis-of-new-2-methylthio-benzog-124-triazolo-15a-quinazolines" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/21894.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">359</span> </span> </div> </div> <div class="card paper-listing mb-3 mt-3"> <h5 class="card-header" style="font-size:.9rem"><span class="badge badge-info">1</span> Synthesis of Quinazoline Derivatives as Selective Inhibitors of Cyclooxygenase-1 Enzyme</h5> <div class="card-body"> <p class="card-text"><strong>Authors:</strong> <a href="https://publications.waset.org/abstracts/search?q=Marcela%20Dvorakova">Marcela Dvorakova</a>, <a href="https://publications.waset.org/abstracts/search?q=Lenka%20Langhansova"> Lenka Langhansova</a>, <a href="https://publications.waset.org/abstracts/search?q=Premysl%20Landa"> Premysl Landa</a> </p> <p class="card-text"><strong>Abstract:</strong></p> A series of quinazoline derivatives bearing aromatic rings in 2- and 4-positions were prepared and tested for their biological activity. Firstly, the compounds were evaluated for their potential to inhibit various kinases, such as autophagy activating kinase ULK1, 3-Phosphoinositide-dependent kinase 1, and TANK-binding kinase 1. None of the compounds displayed any activity on these kinases. Secondly, the compounds were tested for their anti-inflammatory activity expressed as cyclooxygenase (COX) isoforms and 5-lipoxygenase (5-LOX) inhibition. Three of the compounds showed significant selectivity towards COX-1 isoform (COX-2/COX-1 SI = 20-30). They inhibited COX-1 in a single-digit 碌M range. There was also one compound that exhibited inhibitory activity towards all three tested enzymes in 碌M range (IC50COX-1 = 1.9 碌M; IC50COX-2 and 5-LOX = 10.1碌M. COX-1 inhibition was until recently considered undesirable due to COX-1 constitutive expression in most cell types and tissues. Thus, there are not many compounds known with selective COX-1 activity. However, it is now believed that COX-1 plays an important role in the pathophysiology of several acute and chronic disorders, including cancer or neurodegenerative diseases. Thus, the discovery of effective COX-1 selective inhibitors is desirable and important. <p class="card-text"><strong>Keywords:</strong> <a href="https://publications.waset.org/abstracts/search?q=cyclooxygenases" title="cyclooxygenases">cyclooxygenases</a>, <a href="https://publications.waset.org/abstracts/search?q=kinases" title=" kinases"> kinases</a>, <a href="https://publications.waset.org/abstracts/search?q=lipoxygenases" title=" lipoxygenases"> lipoxygenases</a>, <a href="https://publications.waset.org/abstracts/search?q=quinazolines" title=" quinazolines"> quinazolines</a> </p> <a href="https://publications.waset.org/abstracts/116537/synthesis-of-quinazoline-derivatives-as-selective-inhibitors-of-cyclooxygenase-1-enzyme" class="btn btn-primary btn-sm">Procedia</a> <a href="https://publications.waset.org/abstracts/116537.pdf" target="_blank" class="btn btn-primary btn-sm">PDF</a> <span class="bg-info text-light px-1 py-1 float-right rounded"> Downloads <span class="badge badge-light">135</span> </span> </div> </div> </div> </main> <footer> <div id="infolinks" class="pt-3 pb-2"> <div class="container"> <div style="background-color:#f5f5f5;" class="p-3"> <div class="row"> <div class="col-md-2"> <ul class="list-unstyled"> About <li><a href="https://waset.org/page/support">About Us</a></li> <li><a href="https://waset.org/page/support#legal-information">Legal</a></li> <li><a target="_blank" rel="nofollow" href="https://publications.waset.org/static/files/WASET-16th-foundational-anniversary.pdf">WASET celebrates its 16th foundational anniversary</a></li> </ul> </div> <div class="col-md-2"> <ul class="list-unstyled"> Account <li><a href="https://waset.org/profile">My Account</a></li> </ul> </div> <div class="col-md-2"> <ul class="list-unstyled"> Explore <li><a href="https://waset.org/disciplines">Disciplines</a></li> <li><a href="https://waset.org/conferences">Conferences</a></li> <li><a href="https://waset.org/conference-programs">Conference Program</a></li> <li><a href="https://waset.org/committees">Committees</a></li> <li><a href="https://publications.waset.org">Publications</a></li> </ul> </div> <div class="col-md-2"> <ul class="list-unstyled"> Research <li><a href="https://publications.waset.org/abstracts">Abstracts</a></li> <li><a href="https://publications.waset.org">Periodicals</a></li> <li><a href="https://publications.waset.org/archive">Archive</a></li> </ul> </div> <div class="col-md-2"> <ul class="list-unstyled"> Open Science <li><a target="_blank" rel="nofollow" href="https://publications.waset.org/static/files/Open-Science-Philosophy.pdf">Open Science Philosophy</a></li> <li><a target="_blank" rel="nofollow" href="https://publications.waset.org/static/files/Open-Science-Award.pdf">Open Science Award</a></li> <li><a target="_blank" rel="nofollow" href="https://publications.waset.org/static/files/Open-Society-Open-Science-and-Open-Innovation.pdf">Open Innovation</a></li> <li><a target="_blank" rel="nofollow" href="https://publications.waset.org/static/files/Postdoctoral-Fellowship-Award.pdf">Postdoctoral Fellowship Award</a></li> <li><a target="_blank" rel="nofollow" href="https://publications.waset.org/static/files/Scholarly-Research-Review.pdf">Scholarly Research Review</a></li> </ul> </div> <div class="col-md-2"> <ul class="list-unstyled"> Support <li><a href="https://waset.org/page/support">Support</a></li> <li><a href="https://waset.org/profile/messages/create">Contact Us</a></li> <li><a href="https://waset.org/profile/messages/create">Report Abuse</a></li> </ul> </div> </div> </div> </div> </div> <div class="container text-center"> <hr style="margin-top:0;margin-bottom:.3rem;"> <a href="https://creativecommons.org/licenses/by/4.0/" target="_blank" class="text-muted small">Creative Commons Attribution 4.0 International License</a> <div id="copy" class="mt-2">&copy; 2024 World Academy of Science, Engineering and Technology</div> </div> </footer> <a href="javascript:" id="return-to-top"><i class="fas fa-arrow-up"></i></a> <div class="modal" id="modal-template"> <div class="modal-dialog"> <div class="modal-content"> <div class="row m-0 mt-1"> <div class="col-md-12"> <button type="button" class="close" data-dismiss="modal" aria-label="Close"><span aria-hidden="true">&times;</span></button> </div> </div> <div class="modal-body"></div> </div> </div> </div> <script src="https://cdn.waset.org/static/plugins/jquery-3.3.1.min.js"></script> <script src="https://cdn.waset.org/static/plugins/bootstrap-4.2.1/js/bootstrap.bundle.min.js"></script> <script src="https://cdn.waset.org/static/js/site.js?v=150220211556"></script> <script> jQuery(document).ready(function() { /*jQuery.get("https://publications.waset.org/xhr/user-menu", function (response) { jQuery('#mainNavMenu').append(response); });*/ jQuery.get({ url: "https://publications.waset.org/xhr/user-menu", cache: false }).then(function(response){ jQuery('#mainNavMenu').append(response); }); }); </script> </body> </html>

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