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Application of the Pentafluorosulfanyl Group as a Bioisosteric Replacement

机译:五氟氟烷基的施用作为生物话代替代品

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Abstract > The success of fluorinated molecules in drug design has led medicinal chemists to search for new fluorine‐containing substituents. A major recently developed group is the pentafluorosulfanyl group. This group is stable under physiological conditions and displays unique physical and chemical properties. There are currently few synthetic methods to install the SF <sub>5</sub> group, yet efforts to integrate this group into lead optimization continue unabated. Typically, the SF <sub>5</sub> group has been used as a replacement for trifluoromethyl, tert ‐butyl, halogen, or nitro groups. In this review, the use of the SF <sub>5</sub> group as a bioisosteric replacement for each of these three functionalities is compared and contrasted across various groups of biologically active molecules. The organization and presentation of these data should be instructive to medicinal chemists considering to design synthetic strategies to access SF <sub>5</sub> ‐substituted molecules. </abstract> </span> <span class="z_kbtn z_kbtnclass hoverxs" style="display: none;">展开▼</span> </div> <div class="translation abstracttxt"> <span class="zhankaihshouqi fivelineshidden" id="abstract"> <span>机译:</span><Abstract XMLNS =“http://www.wiley.com/namespaces/wiley”type =“main”xml:lang =“en”> <标题类型=“main”>抽象</ title> > 药物设计中的氟化分子的成功使药用化学家寻找新的含氟取代基。最近发达的群体是五氟氟丁基。该组在生理条件下稳定,显示出独特的物理和化学性质。目前有很少的合成方法安装SF <sub> 5 </ sub> 小组,但努力将该组集成为铅优化继续不减。通常,SF <sub> 5 </ sub> 组已被用作三氟甲基的替代品, tert </ i> - 丁基,卤素或硝基。在本次审查中,使用SF <sub> 5 </ sub> 将组作为这些三种功能中的每一个的生物替代品进行比较,并在各种生物活性分子组中进行对比。这些数据的组织和介绍应该对药用化学家来说,考虑到设计综合策略来获得访问SF <sub> 5 </ sub> -substited分子。 </ p> </摘要> </span> <span class="z_kbtn z_kbtnclass hoverxs" style="display: none;">展开▼</span> </div> </div> <div class="record"> <h2 class="all_title" id="enpatent33" >著录项</h2> <ul> <li> <span class="lefttit">来源</span> <div style="width: 86%;vertical-align: text-top;display: inline-block;"> <a href='/journal-foreign-16167/'>《ChemMedChem》</a> <b style="margin: 0 2px;">|</b><span>2017年第18期</span><b style="margin: 0 2px;">|</b><span>共10页</span> </div> </li> <li> <div class="author"> <span class="lefttit">作者</span> <p id="fAuthorthree" class="threelineshidden zhankaihshouqi"> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Sowaileh Munia F.&option=202" target="_blank" rel="nofollow">Sowaileh Munia F.;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Hazlitt Robert A.&option=202" target="_blank" rel="nofollow">Hazlitt Robert A.;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Colby David A.&option=202" target="_blank" rel="nofollow">Colby David A.;</a> </p> <span class="z_kbtnclass z_kbtnclassall hoverxs" id="zkzz" style="display: none;">展开▼</span> </div> </li> <li> <div style="display: flex;"> <span class="lefttit">作者单位</span> <div style="position: relative;margin-left: 3px;max-width: 639px;"> <div class="threelineshidden zhankaihshouqi" id="fOrgthree"> <p>Department of BioMolecular SciencesUniversity of MississippiUniversity MS 38677 USA;</p> <p>Department of Developmental NeurobiologySt. Jude Children's Research HospitalMemphis TN 38105 USA;</p> <p>Department of BioMolecular SciencesUniversity of MississippiUniversity MS 38677 USA;</p> </div> <span class="z_kbtnclass z_kbtnclassall hoverxs" id="zhdw" style="display: none;">展开▼</span> </div> </div> </li> <li > <span class="lefttit">收录信息</span> <span style="width: 86%;vertical-align: text-top;display: inline-block;"></span> </li> <li> <span class="lefttit">原文格式</span> <span>PDF</span> </li> <li> <span class="lefttit">正文语种</span> <span>eng</span> </li> <li> <span class="lefttit">中图分类</span> <span><a href="https://www.zhangqiaokeyan.com/clc/207.html" title="药学">药学;</a></span> </li> <li class="antistop"> <span class="lefttit">关键词</span> <p style="width: 86%;vertical-align: text-top;"> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=bioisosteres&option=203" rel="nofollow">bioisosteres;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=drug design&option=203" rel="nofollow">drug design;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=fluorine&option=203" rel="nofollow">fluorine;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=nitro groups&option=203" rel="nofollow">nitro groups;</a> <a style="color: #3E7FEB;" href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=sulfur&option=203" rel="nofollow">sulfur;</a> </p> <div class="translation"> 机译:Bioisosteres;药物设计;氟;硝基;硫磺; 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