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Synthesis, Characterization, Biological Activity of 4-Oxo-imidazolidin-2-thione Derivatives 4-氧基咪唑烷-2-硫酮衍生物的合成、表征及生物活性研究
Pub Date : 2017-01-01 DOI: 10.3923/CRC.2017.1.13
Amal Mahmoud Yo
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引用次数: 2
Synthesis and spectral study of N,N-diethyl-2-methyl-1-tosylpyrrolidine-2-carboxamide and functionalized sulfonamide scaffolds. N,N-二乙基-2-甲基-1-酰基吡咯烷-2-羧酰胺及功能化磺酰胺支架的合成与光谱研究。
Pub Date : 2016-06-15 DOI: 10.3923/CRC.2016.10.20
O. Ajani, J. D. Udonne, C. Ehi-Eromosele, J. Olugbuyiro, D. Aderohunmu, C. O. Ajanaku, O. Audu
Background and Objective: Sulfonamides are known to represent a class of medicinally important compounds and chemical intermediates, which are extensively used in drug development. The aim of this present study is to synthesize a series of arylsulfonamide-based dialkylated amide motifs. Materials and Methods: In this study, the design and development of arylsulfonamide pharmacophore bearing N,N-diethyl substituted amide moieties 2a-k was achieved in improved yields using non-conventional amidation of p-tolylsulfonamide precursors 1a-k. The structures of the compounds were substantiated based on the results of elemental analysis and spectroscopic data namely, FT-IR, 1H-NMR, 13C-NMR and mass spectra. Results: The series of targeted compounds were synthesized in good to excellent yields and subsequently purified by column chromatography where necessary. Conclusion: The synthesis of arylsulfonamide-based dialkylated amide motifs was successfully achieved. These compounds may serve as versatile intermediates that pave ways toward achieving diverse bioactive heterocyclic compounds for future drug discovery and development.
背景与目的:磺胺类化合物是一类重要的药用化合物和化学中间体,广泛用于药物开发。本研究的目的是合成一系列芳基磺酰胺基二烷基化酰胺基序。材料与方法:本研究通过对甲磺酰胺前体1a-k的非常规酰胺化,实现了含N,N-二乙基取代酰胺2a-k的芳基磺酰胺药效团的设计与开发,提高了收率。根据元素分析和光谱数据(FT-IR, 1H-NMR, 13C-NMR和质谱)证实了化合物的结构。结果:该系列目标化合物的合成收率很高,并在必要时进行柱层析纯化。结论:成功地合成了芳基磺酰胺基二烷基化酰胺基序。这些化合物可以作为多功能中间体,为未来药物的发现和开发铺平道路,以获得多种生物活性杂环化合物。
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引用次数: 0
Electrocoagulation of Azo-2-Naphthol Dye Using Aluminium Electrodes: Effect of Solvent and Kinetics of Adsorption 铝电极电混凝偶氮-2-萘酚染料:溶剂的影响及吸附动力学
Pub Date : 2015-02-01 DOI: 10.3923/CRC.2015.34.43
V. Mkpenie, O. Abakedi
1-Phenylazo-2-naphthol (PAN) was subjected to electrocoagulation using a 0.3 A d.c electrolytic cell in various solvents including ethanol, acetone, benzene and n-hexane. The extent of decolourization of PAN in the solvents has been determined. The highest decolourization was achieved in ethanol with colour removal efficiency of 63% within the first 15 min and 79% after 120 min of electrocoagulation. The decolourization of PAN in the solvents is observed to follow the order: Ethanol>n-hexane>benzene>acetone. The electrocoagulation data has also been interpreted based on adsorption kinetic models. Electrocoagulation of PAN in all the solvents obeyed the pseudo-second order kinetic model and Elovich kinetic model.
采用0.3 a直流电解槽,在乙醇、丙酮、苯和正己烷溶剂中对1-苯基偶氮-2-萘酚(PAN)进行电絮凝。测定了PAN在溶剂中的脱色程度。在乙醇中脱色效果最好,前15分钟脱色率为63%,电凝120分钟后脱色率为79%。PAN在溶剂中的脱色效果为:乙醇>正己烷>苯>丙酮。电凝数据也根据吸附动力学模型进行了解释。聚丙烯腈在各溶剂中的电聚符合准二级动力学模型和Elovich动力学模型。
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引用次数: 5
Synthesis, Characterization and Antibacterial Susceptibility of some Benzenesulfonyl and N-Acetylsulfanilyl Derivatives of Methyl α-D-Glucopyranoside 甲基α- d - glucopyrano苷类苯磺酰基和n -乙酰磺酰基衍生物的合成、表征及抗菌敏感性
Pub Date : 2015-02-01 DOI: 10.3923/CRC.2015.21.33
S. Kawsar, S. Uddin, S. Nishat, M. A. Manchur, Y. Ozeki
A novel regioselective benzenesulphonylation and N-acetylsulfanilylation series of methyl α-D-glucopyranoside derivative (1) has been carried out by direct method and afforded the 6-O-benzenesulfonyl derivative (2) and 6-O-N-acetylsulfanilyl derivative (7) in an excellent yields. In order to obtain newer products, the 6-O-glucopyranoside derivative was further transformed to a series of 2,3,4-tri-O-acyl derivatives (3-6 and 8-11) containing a wide variety of functionalities in a single molecular framework. The structures of the newly synthesized compounds were elucidated with the aid of FTIR, H-NMR spectroscopy and elemental analysis. All the synthesized compounds were also tested for their antibacterial activity against some human pathogenic bacterial microorganisms. For comparative studies, antibacterial activity of standard antibiotics, ampicillin was also carried out against these microorganisms. The study revealed that the acylated products exhibit moderate to good antimicrobial activities. It was interesting to observe that the selected compounds were more sensitive against gram-negative bacteria than that of the gram-positive bacterial strains. We carried out the antibacterial activities of the tested chemicals in vitro. In vivo screening studies of the tested compounds showing promising results will be the subject of our future investigation.
采用直接法对甲基α- d -吡喃葡萄糖苷衍生物(1)进行了新的区域选择性苯磺酰化和n -乙酰磺酰化系列反应,得到了收率较高的6- o -苯磺酰衍生物(2)和6- o - n -乙酰磺酰衍生物(7)。为了获得更新的产品,6- o -葡萄糖吡喃苷衍生物进一步转化为一系列2,3,4-三- o -酰基衍生物(3-6和8-11),在单一分子框架中含有多种功能。通过FTIR、H-NMR和元素分析对新合成化合物的结构进行了表征。并对合成的化合物进行了抑菌活性测试。为了比较研究标准抗生素氨苄西林对这些微生物的抑菌活性。研究表明,酰基化产物具有中等至良好的抗菌活性。有趣的是,所选化合物对革兰氏阴性菌比革兰氏阳性菌更敏感。我们在体外进行了被试化学物质的抗菌活性。在体内筛选研究的测试化合物显示有希望的结果将是我们未来的研究主题。
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引用次数: 3
Phytochemical and Ethnomedicinal Uses of Family Gentianaceae 龙胆科植物化学和民族医药用途
Pub Date : 2015-02-01 DOI: 10.3923/CRC.2015.44.52
D. Chandra, G. Kohli, K. Prasad, G. Bisht, Vinay Deep Punetha, K. S. Khetwal, Manoj Kumar Devrani, H. Pandey
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引用次数: 22
GC-MS Determination of Bioactive Components of Napoleona imperalis P. Beauv 气相色谱-质谱联用法测定帝王拿破仑的生物活性成分
Pub Date : 2015-01-01 DOI: 10.3923/CRC.2015.9.13
C. Chukwu, O. C. Okafor, F. Nwabue, J. Afiukwa, A. Uwakwe
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引用次数: 1
Synthesis of Some New Hydroquinoline and Pyrimido[4,5-b] Quinoline Derivatives 新型对苯二酚和嘧啶[4,5-b]喹啉衍生物的合成
Pub Date : 2015-01-01 DOI: 10.3923/CRC.2015.14.20
A. Ghoneim, M. Assy
A new series of hydroquinolines derivatives (1, 2) have been achieved by the cyclo condensation of 2 (4-methoxybenzylidenemalonitrile), aniline and dimedone in the presence of piperidene. Cyclization of 5,6,7,8-tetrahydro-4-(4-methoxyphenyl)-7,7-dimethyl-5-oxo-2-(phenylamino) quinoline-3-carbonitrile (2) sulphuric acid at room temperature afforded 7,8-dihydro-4-(4methoxyphenyl)-7,7-dimethylquinolin-5(6H)-one[2,3-b]2,3-dihydroquinolin-4 (1H)-one (3). Several substituted pyrimido[4,5-b]quinoline derivatives (4, 5, 6 and 7) were synthesized from 2-amino-1,4,5,6,7,8-hexahydro-4-(4-methoxphenyl)-7,7,-dimethyl-5-oxo-1-phenylquinoline-3carbonitrile (1) via cyclization with thiourea, chloroacetyl chloride, phenyl isothiocynate and formamide, respectively. The condensation of dimedone, with 4-methoxybenzylidene malononitrile in the presence of trimethylamine afforded 11-amino-3,4,8,9-tetrahydro-12-(4-methoxyphenyl)3,3,8,8-tetramethyl-2H-chromeno[2,3-b]quinoline-1, 10(7H,12H)-dione (8) but in ammonium acetate afforded 7,8-dihydro-4-(4-methoxyphenyl)-7,7-dimethylquinolin-5(1H,4H,6H)-one[2,3-b]4-amino-7,8dihydro-7,7-dimethylquinolin-5(6H)-one (9). The structures of the synthesized compounds were elucidated by elemental analyses and spectral data.
在胡椒烯的存在下,通过2(4-甲氧基苄基二聚丙烯腈)、苯胺和二聚酮的环缩合反应,得到了一系列新的对苯二酚衍生物(1,2)。8-tetrahydro-4环合的5、6、7日—(4-methoxyphenyl) 7日7-dimethyl-5-oxo-2——(phenylamino) quinoline-3-carbonitrile(2)硫酸在室温下提供7,8-dihydro-4——(4 methoxyphenyl) 7、7-dimethylquinolin-5(6小时)——(2、3 b) 2, 3-dihydroquinolin-4 (1 h)——(3),几个代替pyrimido(4、5 b)喹啉衍生物(4、5、6和7)是合成2-amino-1, 4, 5, 6, 7, 8-hexahydro-4——(4-methoxphenyl) 7、7,-dimethyl-5-oxo-1-phenylquinoline-3carbonitrile(1)通过与硫脲环合,氯乙酰氯,异硫辛酸苯酯和甲酰胺。双甲酮的缩合,4-methoxybenzylidene丙二腈的三甲胺11-amino-3, 4, 8日9-tetrahydro-12——(4-methoxyphenyl) 3、3、8日8-tetramethyl-2H-chromeno [2, 3 b] quinoline-1, 10 (7 h, 12小时)土卫四(8)但在醋酸铵提供7,8-dihydro-4——(4-methoxyphenyl) 7、7-dimethylquinolin-5 (1 h, 4 h、6 h)——[2,3 b] 4-amino-7 8 dihydro-7 7-dimethylquinolin-5(6小时)——(9)。合成化合物的结构通过元素分析和阐明光谱数据。
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引用次数: 5
Chemical Compositions of Medicinal Mangrove Species Acanthus ilicifolius, Excoecaria agallocha, Rhizophora apiculata and Rhizophora mucronata 红树药用物种刺槐、大褐刺槐、尖根刺槐和细根刺槐的化学成分
Pub Date : 2015-01-01 DOI: 10.3923/CRC.2015.1.8
K. Satyavani, S. Gurudeeban, V. Manigandan, E. Rajamanick, T. Ramanathan
{"title":"Chemical Compositions of Medicinal Mangrove Species Acanthus ilicifolius, Excoecaria agallocha, Rhizophora apiculata and Rhizophora mucronata","authors":"K. Satyavani, S. Gurudeeban, V. Manigandan, E. Rajamanick, T. Ramanathan","doi":"10.3923/CRC.2015.1.8","DOIUrl":"https://doi.org/10.3923/CRC.2015.1.8","url":null,"abstract":"","PeriodicalId":10941,"journal":{"name":"Current Research in Chemistry","volume":"20 1","pages":"1-8"},"PeriodicalIF":0.0,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84766354","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 24
Synthesis of Novel Mannich Bases of Pioglitazone 新型吡格列酮曼尼希碱的合成
Pub Date : 2014-01-01 DOI: 10.3923/CRC.2014.10.15
Ramit Kapoor, R. Arora, Ravinesh Mishra, Manu Arora, Pooja Mittal
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引用次数: 2
Synthesis and Application of Disazo Dyes Derived from 2-amino-5-mercapto-1,3, 4-thiadiazole and 2-chloroaniline on Acrylic Fabric and Nylon 66 Fabric 2-氨基-5-巯基- 1,3,4 -噻二唑和2-氯苯胺双偶氮染料在腈纶和尼龙66织物上的合成及应用
Pub Date : 2014-01-01 DOI: 10.3923/CRC.2014.1.9
J. Otutu, E. M. Efurhievwe, S. U. Ameru
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引用次数: 2
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Current Research in Chemistry
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