Heterocycles最新文献

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Synthesis, Characterization, Molecular Docking Studies and Antimicrobial Activity of Azomethine Derivatives of 1,3-Substituted Pyrazoles 1,3-取代吡唑类亚甲基衍生物的合成、表征、分子对接研究及抗菌活性研究
IF 0.6 4区 化学
Heterocycles Pub Date : 2023-11-02 DOI: 10.3987/com-23-14877
Hissana Ather, Aysha A. Ali Theban, Fareeaa Ashar, Boshra Yahya A. Mohammad Essa, Yomna Ali A. Albarqi, Ghadah Saad A. Alshehri, and Renad Abdulhadi M. Almodawi
{"title":"Synthesis, Characterization, Molecular Docking Studies and Antimicrobial Activity of Azomethine Derivatives of 1,3-Substituted Pyrazoles","authors":"Hissana Ather, Aysha A. Ali Theban, Fareeaa Ashar, Boshra Yahya A. Mohammad Essa, Yomna Ali A. Albarqi, Ghadah Saad A. Alshehri, and Renad Abdulhadi M. Almodawi","doi":"10.3987/com-23-14877","DOIUrl":"https://doi.org/10.3987/com-23-14877","url":null,"abstract":"<span>Two different series of azomethine derivatives of 1,3-substitued pyrazoles were synthesized from the intermediates 3-(4-chlorophenyl)-1-phenyl-1</span><span>H</span><span>-pyrazole-4-carbaldehyde (</span><span>3a</span><span>) and 3-(furan-2-yl)-1-phenyl-1</span><span>H</span><span>-pyrazole-4-carbaldehyde (</span><span>3b</span><span>) by the condensation of various substituted anilines. The intermediates were obtained from the appropriate phenylhydrazones via Vilsmeier–Haack reaction. The synthesized compounds were characterized by IR, </span><span>1</span><span>H NMR and MASS spectral studies. Molecular docking studies results revealed that </span><span>4a7</span><span> and </span><span>4a8</span><span> showed highest binding affinity against fungal target secreted aspartic proteinase (Sap) 1 (</span><span>2QZW</span><span>) and compounds </span><span>4a8</span><span> and </span><span>4a5</span><span> showed highest binding affinity against bacterial target glucosamine-6-phosphate synthase </span><span>(2VF5</span><span>). </span><span>In vitro</span><span> antimicrobial activity of corresponding azomethine derivatives were assessed on Gram-positive and Gram-negative bacteria. Antifungal activity was assessed on </span><span>Candida albicans</span><span>. The results revealed that six out of fifteen compounds screened have shown good antimicrobial activity. Among them, </span><span>4a1</span><span>,</span><span> 4a4</span><span>,</span><span> 4a6 </span><span>and</span><span> 4a7</span><span> shown good inhibition against </span><span>Candida albicans</span><span>.</span>","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138542650","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of New Glycoluril Derivatives via Ring-Closing Metathesis 合环复合法合成新的甘醇衍生物
IF 0.6 4区 化学
Heterocycles Pub Date : 2023-11-02 DOI: 10.3987/com-23-14912
Sambasivarao Kotha and Deepshikha Singh
{"title":"Synthesis of New Glycoluril Derivatives via Ring-Closing Metathesis","authors":"Sambasivarao Kotha and Deepshikha Singh","doi":"10.3987/com-23-14912","DOIUrl":"https://doi.org/10.3987/com-23-14912","url":null,"abstract":"<span>Tetra-</span><span>N</span><span>-allylation of glycoluril reactions followed by ring-closing metathesis has been used to generate new concave-shaped glycoluril derivatives. The advantages of this method are mild conditions, single-product formation and good yield.<br/></span>","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138495427","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Diastereoselective Synthesis of 2,8-Dioxabicyclo[3.3.1]Nonane Derivatives via I 1,2 -二氧杂环[3.3.1]壬烷衍生物的非对映选择性合成
IF 0.6 4区 化学
Heterocycles Pub Date : 2023-11-01 DOI: 10.3987/com-23-14891
-Mediated Cascade Reactions
{"title":"Diastereoselective Synthesis of 2,8-Dioxabicyclo[3.3.1]Nonane Derivatives via I","authors":"-Mediated Cascade Reactions","doi":"10.3987/com-23-14891","DOIUrl":"https://doi.org/10.3987/com-23-14891","url":null,"abstract":"<span>The highly diastereoselective one-pot synthesis generating a variety of 9,9-dimethyl-2,8-dioxabicyclo[3.3.1]nonane derivatives up to </span><span>dr</span><span> &gt;19:1 has been established by the reaction of a 2’-methoxylchalcone with isobutyraldehyde via a spontaneous sequential one-pot Michael addition/aldol reaction/demethylative bicyclization in the presence of molecular iodine. </span>","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138495426","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Briastecholide N: a New Chlorine-Containing Briarane Diterpenoid Deriving from Cultured Briastecholide N:一种新的含氯Briarane二萜
IF 0.6 4区 化学
Heterocycles Pub Date : 2023-10-30 DOI: 10.3987/com-23-14911
You-Ying Chen, Yueh-Wen Liu, Su-Ying Chien, Yu-Cheng Chen, Fu-Ching Chiu, Po-Wei Huang, I-Li Su, Zhi-Hong Wen, Hung-Tsung Lee, and Ping-Jyun Sung
{"title":"Briastecholide N: a New Chlorine-Containing Briarane Diterpenoid Deriving from Cultured","authors":"You-Ying Chen, Yueh-Wen Liu, Su-Ying Chien, Yu-Cheng Chen, Fu-Ching Chiu, Po-Wei Huang, I-Li Su, Zhi-Hong Wen, Hung-Tsung Lee, and Ping-Jyun Sung","doi":"10.3987/com-23-14911","DOIUrl":"https://doi.org/10.3987/com-23-14911","url":null,"abstract":"<span>A new chlorine-containing briarane-type diterpenoid, briastecholide N (</span><span>1</span><span>) was isolated from cultured octocoral </span><span>Briareum stechei</span><span> </span><span>via</span><span> chemical screening. The structure of </span><span>1</span><span> was corroborated by 2D NMR experiments and confirmed backed by single-crystal X-ray diffraction analysis. The study found that </span><span>1</span><span> is capable of increasing the release of alkaline phosphatse (ALP) at </span><span>10 μM.</span><span><br/></span>","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-10-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138495425","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthetic Studies toward 11- 对11-的综合研究
IF 0.6 4区 化学
Heterocycles Pub Date : 2023-10-24 DOI: 10.3987/rev-23-1018
-Debenzoyltashironin
{"title":"Synthetic Studies toward 11-","authors":"-Debenzoyltashironin","doi":"10.3987/rev-23-1018","DOIUrl":"https://doi.org/10.3987/rev-23-1018","url":null,"abstract":"<span>11-</span><span>O</span><span>-Debenzoyltashironin is a highly oxygenated </span><span>allo</span><span>-cedrane sesquiterpenoid with seven contiguous chiral centers in a compact fused ring, and shows remarkable neurite extension activity. Total syntheses of the title and related compounds are reviewed.</span>","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138495424","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A Facile Synthesis and Anticancer Activity of ( ()的简易合成及其抗癌活性
IF 0.6 4区 化学
Heterocycles Pub Date : 2023-10-18 DOI: 10.3987/com-23-14909
)-Diethyl 2-Styrylquinoline-3,4-dicarboxylates
{"title":"A Facile Synthesis and Anticancer Activity of (","authors":")-Diethyl 2-Styrylquinoline-3,4-dicarboxylates","doi":"10.3987/com-23-14909","DOIUrl":"https://doi.org/10.3987/com-23-14909","url":null,"abstract":"<span>In the present investigation, a simple and flexible synthesis of a series of novel (</span><span>E</span><span>)-diethyl 2-styrylquinoline-3,4-dicarboxylates </span><span>3a-q</span><span> has been achieved for the first time in good yields, involving one-pot sequential Arbuzov/Horner–Emmons reaction sequence using the newly-synthesized diethyl 2-(bromomethyl)quinoline-3,4-dicarboxylate as the substrate. The latter was obtained by NBS-mediated radical bromination reaction of the readily available diethyl 2-methylquinoline-3,4-dicarboxylate. A primary </span><span>in vitro </span><span>evaluation for their antiproliferative activity against human cancer cell lines (A549, HT29 and T24) revealed that the compound </span><span>3k</span><span> with 3,4,5-trimethoxystyryl moiety represented the most active molecule against the tested A549 cell lines in this round of effort with the IC</span><span>50</span><span> values of 2.38 µmol•L</span><span>-1</span><span>, being higher than the reference cisplatin.</span>","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138495423","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Simultaneous Denitrative C–C Bond Formation and Construction of Pyrazole Ring Leading to 1,1'-Diphenyl-4,4'-bipyrazole 同时反硝化C-C键形成和吡唑环的构建导致1,1'-二苯基-4,4'-联吡唑
IF 0.6 4区 化学
Heterocycles Pub Date : 2023-01-01 DOI: 10.3987/com-22-14772
N. Nishiwaki, Kento Iwai, Nana Hatayama
{"title":"Simultaneous Denitrative C–C Bond Formation and Construction of Pyrazole Ring Leading to 1,1'-Diphenyl-4,4'-bipyrazole","authors":"N. Nishiwaki, Kento Iwai, Nana Hatayama","doi":"10.3987/com-22-14772","DOIUrl":"https://doi.org/10.3987/com-22-14772","url":null,"abstract":"–  -Formyl-  -nitroenamine reacts with phenylhydrazine to afford 1,1'-diphenyl-4,4'-bipyrazole. The unusual C–C bond formation was found to proceed in an ionic mechanism initiated by excess amount of hydrazine. This reaction is interesting from a viewpoint of synthetic chemistry because it simultaneously involves the construction of a pyrazole ring and the formation of a C–C bond under neutral conditions.  -Formyl-","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"70398879","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A New Compound Embeloside A with Hypoglycemic Potential from the Fruits of Embelia Oblongifolia Hemsl. 从桔梗果实中提取具有降血糖作用的新化合物桔梗苷A。
IF 0.6 4区 化学
Heterocycles Pub Date : 2023-01-01 DOI: 10.3987/com-22-14799
Lei Yu, Haifeng Wang, Yuqing Sun, Ying Xu, Bing Liu, Ning Chen, Yingjie Liu, Dongxue Wang
{"title":"A New Compound Embeloside A with Hypoglycemic Potential from the Fruits of Embelia Oblongifolia Hemsl.","authors":"Lei Yu, Haifeng Wang, Yuqing Sun, Ying Xu, Bing Liu, Ning Chen, Yingjie Liu, Dongxue Wang","doi":"10.3987/com-22-14799","DOIUrl":"https://doi.org/10.3987/com-22-14799","url":null,"abstract":"","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"70399215","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Organic Base-Catalyzed Cascade Reaction of Electron-Deficient Cyclopentadienone with Prop-2-yn-1-ols: Formation of 3-Methylenetetrahydrofuran Ring Condensed with Cyclopentenone 有机碱催化缺电子环戊二酮与丙-2-炔-1-醇的级联反应:与环戊烯酮缩合形成3-亚甲基四氢呋喃环
IF 0.6 4区 化学
Heterocycles Pub Date : 2023-01-01 DOI: 10.3987/com-23-14811
K. Yamaguchi
{"title":"Organic Base-Catalyzed Cascade Reaction of Electron-Deficient Cyclopentadienone with Prop-2-yn-1-ols: Formation of 3-Methylenetetrahydrofuran Ring Condensed with Cyclopentenone","authors":"K. Yamaguchi","doi":"10.3987/com-23-14811","DOIUrl":"https://doi.org/10.3987/com-23-14811","url":null,"abstract":"procedure, bicyclic compounds","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"70400838","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis and Biological Evaluation of 5-Methylpyrimidine Derivatives as Dual Inhibitors of EGFR and Src for Cancer Treatment 5-甲基嘧啶衍生物作为EGFR和Src双重抑制剂治疗癌症的合成和生物学评价
IF 0.6 4区 化学
Heterocycles Pub Date : 2023-01-01 DOI: 10.3987/com-23-14824
Longjia Yan, Yaqing Zuo, Kehui Chen, Ying Xu, Y. Le
{"title":"Synthesis and Biological Evaluation of 5-Methylpyrimidine Derivatives as Dual Inhibitors of EGFR and Src for Cancer Treatment","authors":"Longjia Yan, Yaqing Zuo, Kehui Chen, Ying Xu, Y. Le","doi":"10.3987/com-23-14824","DOIUrl":"https://doi.org/10.3987/com-23-14824","url":null,"abstract":"","PeriodicalId":13166,"journal":{"name":"Heterocycles","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"70401116","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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