Design, synthesis of tri‐substituted pyrazole derivatives as promising antimicrobial agents and investigation of structure activity relationships

Reddy Guda Mallikarjuna; Garcia Jarem Raul; Yuvaraja Gutha; Venkata Subbaiah Munagapati; Wen Jet‐Chau

摘要

Abstract >The major diseases spread in the environment only because of microbes. Even, intensive care units in the hospitals are polluted by microorganisms, particularly, Gram‐positive bacteria. Although many antibiotics are existed, there is a need to develop up to date microbial‐resistant agents. Hence, the current study aimed to develop prominent antimicrobial drug‐related compounds. Thus, a novel series of tri‐substituted analogs and their intermediates were synthesized. In addition, total new compounds were screened for their antimicrobial assay and identified as the most efficient biologically active compounds. Moreover, minimal inhibitory antimicrobial activity and appropriate structure activity relationships were investigated. From the results it was observed that, viability of Gram‐positive bacteria was most powerfully affected by all active compounds. Finally, this research demonstrated that, these biologically energetic amalgams can be utilized for further preclinical studies with the ambition of standing unique inventive drugs. </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 Type =“Main”XML：Lang =“en”> <标题类型=“main”>抽象</ title> >主要疾病仅因微生物而在环境中传播。即使，医院的重症监护病房均由微生物污染，特别是革兰氏阳性细菌。虽然存在许多抗生素，但需要开发最新的微生物抗性剂。因此，目前的研究旨在发展突出的抗微生物药物相关化合物。因此，合成了一种新型的三级取代类似物及其中间体。此外，筛选新化合物的抗微生物测定并鉴定为最有效的生物活性化合物。此外，研究了最小的抑制性抗微生物活性和适当的结构活性关系。从结果观察到，革兰氏阳性细菌的活力最有力地受到所有活性化合物的影响。最后，这项研究表明，这些生物学上能量汞合金可用于进一步临界研究，以野心的独特本发明药物的野心。</ 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-34660/'>《Journal of Heterocyclic Chemistry: The International Journal of Heterocyclic Chemistry》</a> <b style="margin: 0 2px;">|</b><span>2020年第5期</span><b style="margin: 0 2px;">|</b><span>共9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=Reddy Guda Mallikarjuna&option=202" target="_blank" rel="nofollow">Reddy Guda Mallikarjuna;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Garcia Jarem Raul&option=202" target="_blank" rel="nofollow">Garcia Jarem Raul;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Yuvaraja Gutha&option=202" target="_blank" rel="nofollow">Yuvaraja Gutha;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Venkata Subbaiah Munagapati&option=202" target="_blank" rel="nofollow">Venkata Subbaiah Munagapati;</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Wen Jet‐Chau&option=202" target="_blank" rel="nofollow">Wen Jet‐Chau;</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>Ural Federal University Chemical Engineering InstituteYekaterinburg Russian Federation;</p> <p>Department of ChemistryState University of Ponta GrossaPonta Grossa Brazil;</p> <p>Guangdong Provincial Key Laboratory for Radionuclides Pollution Control and Resources School of Environmental Science and EngineeringGuangzhou UniversityGuangzhou China;</p> <p>Research Centre for Soil &</p> <p>Water Resources and Natural Disaster Prevention (SWAN)National Yunlin University of Science &</p> <p>TechnologyDouliou Taiwan Republic of China;</p> <p>Research Centre for Soil &</p> <p>Water Resources and Natural Disaster Prevention (SWAN)National Yunlin University of Science &</p> <p>TechnologyDouliou Taiwan Republic of China;</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/1184.html" title="有机化学">有机化学;</a></span> </li> <li class="antistop"> <span class="lefttit">关键词</span> <p style="width: 86%;vertical-align: text-top;"> </p> </li> </ul> </div> </div> <div class="literature cardcommon"> <div class="similarity "> <h3 class="all_title" id="enpatent66">相似文献</h3> <div class="similaritytab clearfix"> <ul> <li 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Haowu Jia</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=贾浩武&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor">,贾浩武</a> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=Wei Li&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor">,Wei Li</a> <span> <a href="/conference-cn-66221/" target="_blank" rel="nofollow" class="tuijian_authcolor"> . 2017年上海市化学化工学会农用化学专业委员会年会暨上海市肥料农药行业协会专题研讨会 </a> <span> <span> . 2017</span> </span> </div> </li> <li> <div> <b>7. </b><a class="enjiyixqcontent" href="/academic-degree-domestic_mphd_thesis/020314316946.html">生物活性有机物及有机/无机杂化分子的研究：（Ⅰ）：双酰基硫脲的合成、生物活性及晶体结构研究;（Ⅱ）：3，6-二取代-1，2，4-三唑并[3，4-b]噻二唑的合成与生物活性测定;（Ⅲ）：六钼酸芳香亚胺衍生物的合成及晶体结构研究</a> <b>[A] </b> <span> <a href="/search.html?doctypes=4_5_6_1-0_4-0_1_2_3_7_9&sertext=蔡志娟&option=202" target="_blank" rel="nofollow" class="tuijian_auth tuijian_authcolor"> . 蔡志娟</a> <span> . 2007</span> </span> </div> </li> </ul> <ul style="display: none;"> <li> <div> <b>1. </b><a class="enjiyixqcontent" href="/patent-detail/06120101040991.html">一类具有抗肿瘤活性的3,5-二苯基取代的二氢吡唑类衍生物及合成方法和应用</a> <b>[P]</b> . <span> 中国专利： CN110128342A </span> <span> . 2019-08-16</span> </div> </li> <li> <div> <b>2. </b><a class="enjiyixqcontent" href="/patent-detail/06120106000213.html">吡唑并N-取代去甲去氢斑蝥素酰亚胺衍生物及其合成方法、活性测试方法与应用</a> <b>[P]</b> . <span> 中国专利： CN101812066A </span> <span> . 2010-08-25</span> </div> </li> <li> <div> <b>3. </b><a class="enjiyixqcontent" href="/patent-detail/06130454817128.html">SUBSTITUTED PYRAZOLE DERIVATIVE, ITS PRODUCTION AND ANTIMICROBIAL AGENT CONTAINING THE DERIVATIVE AS ACTIVE INGREDIENT AND USEFUL FOR AGRICULTUTE AND HORTICULTURE</a> <b>[P]</b> . <span> 外国专利：  JPH10168063A </span> <span> . 1998-06-23</span> </div> <p class="zwjiyix translation" style="max-width: initial;height: auto;word-break: break-all;white-space: initial;text-overflow: initial;overflow: initial;"> <span>机译：取代的吡唑衍生物，其生产和包含该衍生物作为活性成分且对农业和园艺有用的抗微生物剂 </span> </p> </li> <li> <div> <b>4. </b><a class="enjiyixqcontent" href="/patent-detail/06130455379938.html">Substituted pyrazolyl-pyrazole derivatives, processes for their preparation and their use as herbicides (SUBSTITUTED PYRAZOLYL-PYRAZOLE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR USE AGENTS WITH HERBICIDAL ACTION)</a> <b>[P]</b> . <span> 外国专利：  KR970706281A </span> <span> . 1997-11-03</span> </div> <p class="zwjiyix translation" style="max-width: initial;height: auto;word-break: break-all;white-space: initial;text-overflow: initial;overflow: initial;"> <span>机译：取代的吡唑基-吡唑衍生物，其制备方法及其作为除草剂的用途（取代的吡唑基-吡唑衍生物，其制备方法及其具有除草作用的使用剂） </span> </p> </li> <li> <div> <b>5. </b><a class="enjiyixqcontent" href="/patent-detail/06130456854721.html">Substituted pyrazolyl-pyrazole derivatives, process for their preparation and their use as agents with herbicidal activity</a> <b>[P]</b> . <span> 外国专利：  DE4435373A1 </span> <span> . 1996-03-28</span> </div> <p class="zwjiyix translation" style="max-width: initial;height: auto;word-break: break-all;white-space: initial;text-overflow: initial;overflow: initial;"> <span>机译：取代的吡唑基-吡唑衍生物，其制备方法及其用作除草剂的用途 </span> </p> </li> </ul> </div> </div> </div> <div class="theme cardcommon" style="overflow: auto;display:none"> <h3 class="all_title" id="enpatent55">相关主题</h3> <ul id="subject"> </ul> </div> </div> </div> </div> <div class="right rightcon"> <div class="details_img cardcommon clearfix" style="margin-bottom: 10px;display:none;" > </div> </div> </div> <div id="thesis_get_original1" class="downloadBth" style="bottom: 19px;z-index: 999;" onclick="ywcd('0704025586099','4',7,2,1,'',this,24)" class="delivery" prompt="010401" title="通过人工服务将文献原文发送至邮箱" >获取原文</div> <div class="journalsub-pop-up" style="display: none"> <div class="journal-sub"> <h2>期刊订阅</h2> <img src="https://cdn.zhangqiaokeyan.com/img/loginclose.png" alt="关闭" onclick="$('.journalsub-pop-up').hide()"> <p 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