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Heterocyclic Communications最新文献

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Cytotoxic and antimicrobial activities of some novel heterocycles employing 6-(1,3-diphenyl-1H-pyrazol-4-yl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile 新型杂环6-(1,3-二苯基- 1h -吡唑-4-基)-4-氧-2-硫氧-1,2,3,4-四氢嘧啶-5-碳腈的细胞毒性和抗菌活性
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2019-01-01 DOI: 10.1515/hc-2019-0008
S. K. Ramadan, E. El‐Helw, H. A. Sallam
{"title":"Cytotoxic and antimicrobial activities of some novel heterocycles employing 6-(1,3-diphenyl-1H-pyrazol-4-yl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile","authors":"S. K. Ramadan, E. El‐Helw, H. A. Sallam","doi":"10.1515/hc-2019-0008","DOIUrl":"https://doi.org/10.1515/hc-2019-0008","url":null,"abstract":"Abstract A pyrimidinethione derivative namely, 6-(1,3-diphenyl-1H-pyrazol-4-yl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile, was readily synthesized and reacted with carbon electrophiles in an attempt to synthesize selected fused heterocycles. The reactivity of 6-(1,3-diphenyl-1H-pyrazol-4-yl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile was investigated towards selected nitrogen nucleophiles. Thiation and hydrolysis reactions of the tetrahydropyrimidine derivative were investigated. Antitumor and antimicrobial activity evaluation of some of the synthesized products exhibited promising results.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"25 1","pages":"107 - 115"},"PeriodicalIF":2.3,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1515/hc-2019-0008","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43452584","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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: 25
Synthesis and AChE inhibitory activity of N-glycosyl benzofuran derivatives N-糖基苯并呋喃衍生物的合成及其乙酰胆碱酯酶抑制活性
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2019-01-01 DOI: 10.1515/hc-2019-0021
Yu-Ran Wu, Shu-Ting Ren, Lei Wang, Xiu-Jian Liu, You-Xian Wang, Shu-Hao Liu, Wei-wei Liu, D. Shi, Zhi-ling Cao
{"title":"Synthesis and AChE inhibitory activity of N-glycosyl benzofuran derivatives","authors":"Yu-Ran Wu, Shu-Ting Ren, Lei Wang, Xiu-Jian Liu, You-Xian Wang, Shu-Hao Liu, Wei-wei Liu, D. Shi, Zhi-ling Cao","doi":"10.1515/hc-2019-0021","DOIUrl":"https://doi.org/10.1515/hc-2019-0021","url":null,"abstract":"Abstract Six N-glycosyl benzofuran derivatives were synthesized by the catalysis of organic bases and condensation agents. The benzofuran derivatives were obtained by the reaction of various salicylaldehydes in acetone, and then hydrolyzed to the corresponding carboxylic acids. Finally, the target compounds were synthesized by acylation and the reaction conditions were optimized. The acetylcholinesterase (AChE) inhibitory activity of the desired compounds was tested using Ellman’s method. Most of the compounds showed acetylcholinesterase-inhibition activity; N-(2,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)benzofuran-2-carbxamide (5a) showed the best acetylcholinesterase inhibition, with an inhibitory rate of 84%.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"25 1","pages":"162 - 166"},"PeriodicalIF":2.3,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1515/hc-2019-0021","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47450883","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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: 1
Synthesis of 1,2,3 triazole-linked benzimidazole through a copper-catalyzed click reaction 铜催化点击反应合成1,2,3-三唑连接的苯并咪唑
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2019-01-01 DOI: 10.1515/hc-2019-0016
M. Bakherad, Ali Keivanloo, A. Amin, Amir Farkhondeh
{"title":"Synthesis of 1,2,3 triazole-linked benzimidazole through a copper-catalyzed click reaction","authors":"M. Bakherad, Ali Keivanloo, A. Amin, Amir Farkhondeh","doi":"10.1515/hc-2019-0016","DOIUrl":"https://doi.org/10.1515/hc-2019-0016","url":null,"abstract":"Abstract An efficient method has been developed for the synthesis of 1,2,3 triazole-linked benzimidazole through a copper-catalyzed click reaction in ethanol at 50°C. A broad range of aromatic azides were successfully reacted with n-propynylated benzimidazole via copper-catalyzed azide-alkyne cycloaddition reactions in the absence of a ligand. This method offers many advantages including short reaction times, low cost, and simple purification procedures.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"25 1","pages":"122 - 129"},"PeriodicalIF":2.3,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1515/hc-2019-0016","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43951888","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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: 6
Synthesis and fungicidal activities of perfluoropropan-2-yl-based novel quinoline derivatives 基于全氟丙烷-2-基的新型喹啉衍生物的合成及抑菌活性研究
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2019-01-01 DOI: 10.1515/hc-2019-0002
Zai Zhang, Minhua Liu, Weidong Liu, J. Xiang, Jianming Li, Zhong Li, Xingping Liu, Mingzhi Huang, Aiping Liu, Xingliang Zheng
{"title":"Synthesis and fungicidal activities of perfluoropropan-2-yl-based novel quinoline derivatives","authors":"Zai Zhang, Minhua Liu, Weidong Liu, J. Xiang, Jianming Li, Zhong Li, Xingping Liu, Mingzhi Huang, Aiping Liu, Xingliang Zheng","doi":"10.1515/hc-2019-0002","DOIUrl":"https://doi.org/10.1515/hc-2019-0002","url":null,"abstract":"Abstract A series of novel perfluoropropan-2-yl-based quinoline derivatives was designed and synthesized utilizing tebufloquin as the lead compound. The structures of all the newly synthesized compounds were confirmed by spectroscopic data 1HNMR, MS and elemental analysis. The results of bioassay indicated that these compounds exhibited potent fungicidal activities against Erysiphe graminis. Especially, compound 8c displayed excellent activity with EC50 value at 1.48 mg / L, which was better than that of the commercialized fungicide --- tebufloquin. The structure-activity relationship for these new compounds was also discussed.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"25 1","pages":"91 - 97"},"PeriodicalIF":2.3,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1515/hc-2019-0002","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47981731","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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: 6
Theoretical study of the formation of a spiro-Sn-heterocyclic compound by cycloaddition reaction of Me2C=Sn: and ethene Me2C=Sn:与乙烯环加成反应生成螺-Sn杂环化合物的理论研究
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2018-12-19 DOI: 10.1515/hc-2018-0129
Xiaojun Tan, Xiuhui Lu
{"title":"Theoretical study of the formation of a spiro-Sn-heterocyclic compound by cycloaddition reaction of Me2C=Sn: and ethene","authors":"Xiaojun Tan, Xiuhui Lu","doi":"10.1515/hc-2018-0129","DOIUrl":"https://doi.org/10.1515/hc-2018-0129","url":null,"abstract":"Abstract X2C=Sn: compounds (X=H, Me, F, Cl, Br, Ph, Ar) are new species. The cycloaddition reactions of X2C=Sn: are also a new study field of unsaturated stannylene chemistry. The mechanism of cycloaddition reaction between singlet Me2C=Sn: and ethene was investigated for the first time using the MP2/GENECP (C, H in 6-311++G**; Sn in LanL2dz) method. From the potential energy profile, it was predicted that the reaction has one dominant channel in which the 5p unoccupied orbital of Sn: in Me2C=Sn: and the π orbital of ethene form a π→p donor-acceptor bond in an intermediate product. Instability of the intermediate product results in its isomerization to a four-membered ring of stannylene. The four-membered stannylene further combines with ethene to form another intermediate product that further isomerizes to a spiro-Sn-heterocyclic ring compound.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"24 1","pages":"311 - 315"},"PeriodicalIF":2.3,"publicationDate":"2018-12-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1515/hc-2018-0129","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41533995","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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: 1
Microwave-assisted synthesis of quinazolin-4(3H)-ones catalyzed by SbCl3 SbCl3催化喹唑啉-4(3H)-的微波辅助合成
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2018-12-19 DOI: 10.1515/hc-2018-0115
Hua-Jie Kang, Weili Wang, Qinqian Sun, Shuya Yang, Juan Jin, Xuewen Zhang, Xiaoliang Ren, Jiming Zhang, Jianhua Zhou
{"title":"Microwave-assisted synthesis of quinazolin-4(3H)-ones catalyzed by SbCl3","authors":"Hua-Jie Kang, Weili Wang, Qinqian Sun, Shuya Yang, Juan Jin, Xuewen Zhang, Xiaoliang Ren, Jiming Zhang, Jianhua Zhou","doi":"10.1515/hc-2018-0115","DOIUrl":"https://doi.org/10.1515/hc-2018-0115","url":null,"abstract":"Abstract Antimony(III) trichloride (SbCl3) is an effective catalyst (1 mol%) for the condensation of anthranilic amide with various aldehydes or ketones to quinazolin-4(3H)-one derivatives in good to excellent yields under microwave irradiation. The process is carried out within several minutes under solvent-free conditions. This general methodology has the advantages of simplicity, mild reaction conditions and high yields of products.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"24 1","pages":"293 - 296"},"PeriodicalIF":2.3,"publicationDate":"2018-12-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1515/hc-2018-0115","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44318963","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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: 8
5-Bromo-1-(4-chlorobenzyl)-1H-indole-2-carboxamides as new potent antibacterial agents 5-溴-1-(4-氯苯)- 1h -吲哚-2-羧胺类新型高效抗菌剂
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2018-12-19 DOI: 10.1515/hc-2018-0107
Y. Mane, Smita S. Patil, D. Biradar, B. Khade
{"title":"5-Bromo-1-(4-chlorobenzyl)-1H-indole-2-carboxamides as new potent antibacterial agents","authors":"Y. Mane, Smita S. Patil, D. Biradar, B. Khade","doi":"10.1515/hc-2018-0107","DOIUrl":"https://doi.org/10.1515/hc-2018-0107","url":null,"abstract":"Abstract Ten 5-bromoindole-2-carboxamides were synthesized, characterized and evaluated for antibacterial activity against pathogenic Gram-negative bacteria Klebsiella pneumoniae, Escherichia coli, Pseudomonas aeruginosa and Salmonella Typhi using gentamicin and ciprofloxacin as internal standards. Compounds 7a–c, 7g and 7h exhibit high antibacterial activity with a minimum inhibitory concentration (MIC) of 0.35–1.25 μg/mL. Compounds 7a–c exhibit antibacterial activities that are higher than those of the standards against E. coli and P. aeruginosa.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"54 4","pages":"327 - 332"},"PeriodicalIF":2.3,"publicationDate":"2018-12-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1515/hc-2018-0107","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41245154","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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: 4
Diaminomaleonitrile as a versatile building block for the synthesis of 4,4′-biimidazolidinylidenes and 4,4′-bithiazolidinylidenes 二氨基甲基丙烯腈作为合成4,4′-双咪唑烷亚基和4,4′–双噻唑烷亚基的通用构建基
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2018-12-19 DOI: 10.1515/hc-2018-0127
Mahsa Doomanlou, H. Kabirifard, M. Asadi, M. Moloudi, S. S. Mirfazli
{"title":"Diaminomaleonitrile as a versatile building block for the synthesis of 4,4′-biimidazolidinylidenes and 4,4′-bithiazolidinylidenes","authors":"Mahsa Doomanlou, H. Kabirifard, M. Asadi, M. Moloudi, S. S. Mirfazli","doi":"10.1515/hc-2018-0127","DOIUrl":"https://doi.org/10.1515/hc-2018-0127","url":null,"abstract":"Abstract Ring closure reactions of diaminomaleonitrile (DAMN) with electrophilic aryl isocyanates and aryl isothiocyanates lead to the formation of the target 5,5′-diimino-1,1′-diaryl-4,4′-biimidazolidinylidene-2,2′-diones 2a,b and 2,2′-diarylimino-4,4′-bithiazolidinylidenes 4a–e, respectively. The protocol provides a new strategy for the synthesis of a wide range of alkenes with two electron-donating and two withdrawing substituents of DAMN in moderate to good yields.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"24 1","pages":"303 - 306"},"PeriodicalIF":2.3,"publicationDate":"2018-12-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1515/hc-2018-0127","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44750054","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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
Urea nitrate catalyzed synthesis of 2-arylbenzothiazoles using the grindstone technique 磨刀石法催化硝酸脲合成2-芳基苯并噻唑
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2018-12-19 DOI: 10.1515/hc-2018-0133
Divyani Gandhi, S. Agarwal
{"title":"Urea nitrate catalyzed synthesis of 2-arylbenzothiazoles using the grindstone technique","authors":"Divyani Gandhi, S. Agarwal","doi":"10.1515/hc-2018-0133","DOIUrl":"https://doi.org/10.1515/hc-2018-0133","url":null,"abstract":"Abstract An efficient, green and environmentally friendly grindstone method for the synthesis of 2-arylbenzothiazole derivatives in the presence of urea nitrate as the catalyst under solvent-free conditions was developed. All products were characterized by elemental analysis and spectral methods.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"24 1","pages":"307 - 310"},"PeriodicalIF":2.3,"publicationDate":"2018-12-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1515/hc-2018-0133","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44045414","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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: 8
An efficient synthesis of imidazo[2,1-b][1,3,4]thiadiazol-7-ium hydroxides by a one-pot, three-component reaction in water 一锅三组分反应合成咪唑[2,1-b][1,3,4]噻二唑-7-ium氢氧化物
IF 2.3 3区 化学
Heterocyclic Communications Pub Date : 2018-12-19 DOI: 10.1515/hc-2018-0117
J. Khalafy, Nasser Etivand, Neda Khalillou
{"title":"An efficient synthesis of imidazo[2,1-b][1,3,4]thiadiazol-7-ium hydroxides by a one-pot, three-component reaction in water","authors":"J. Khalafy, Nasser Etivand, Neda Khalillou","doi":"10.1515/hc-2018-0117","DOIUrl":"https://doi.org/10.1515/hc-2018-0117","url":null,"abstract":"Abstract An improved synthesis of 2-ethyl-5-(2-hydroxy-4-oxoquinolin-3(4H)-ylidene)-6-aryl-5,6-dihydroimidazo[2,1-b][1,3,4]thiadiazol-7-ium hydroxide derivatives 4a–k via the reaction of aryl glyoxal monohydrates 1a–k, quinoline-2,4-diol 2 and 2-amino-[1,3,4]thiadiazole (3) in the presence of Et3N/sulfamic acid in H2O is described. This green protocol is characterized by the use of the readily available catalyst and reactants, short reaction times, operational simplicity and high yields of products. The structures of all compounds were characterized by 1H NMR, 13C NMR and Fourier-transform infrared (FT-IR) spectral data and microanalyses.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"24 1","pages":"297 - 302"},"PeriodicalIF":2.3,"publicationDate":"2018-12-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1515/hc-2018-0117","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49003941","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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: 4
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