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Synthesis and Anti Convulsant Activity of Novel Oxadiazole Substituted Phenothiazine Derivatives 新型恶二唑取代吩噻嗪衍生物的合成及其抗惊厥活性
Pub Date : 2021-05-05 DOI: 10.9734/BPI/CACB/V4/1783F
Dighe Ns, Bankar Aa, DS Musmade, S. Nirmal
The research is directed towards the synthesis and evaluation of novel agents for the treatment of various neurological disorders. The phenothiazine nucleus has been well explored for the various biological activities in past. The oxadiazole substituted phenothiazine have been of keen interest as a drug candidate for the treatment of various neurological disorders. In view of these an attempt has been made to synthesize substituted phenothiazine and explore them for promising anti convulsant activity. The anti-convulsant activity of synthesized compounds had been done by using Strychnine induced and 4-amino pyridine induced models.
该研究旨在合成和评估治疗各种神经系统疾病的新型药物。过去人们对吩噻嗪核的各种生物活性进行了很好的探索。恶二唑取代吩噻嗪作为一种治疗各种神经系统疾病的候选药物已引起人们的浓厚兴趣。鉴于此,本文尝试合成取代吩噻嗪并探索其抗惊厥活性。采用士的宁诱导模型和4-氨基吡啶诱导模型对合成的化合物进行抗惊厥活性测定。
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引用次数: 1
Polymeric Composite Materials Based on Silicate: I-Synthesis, Characterization and Formation Mechanism 硅酸盐高分子复合材料的合成、表征及形成机理
Pub Date : 2018-01-23 DOI: 10.26671/IJIRG.2017.3.6.102
A. Mm, M. Abass, A. B. Ibrahim, E. S. Zakaria, A. Hassan
Magneso-silicate has been synthesized by precipitation technique. Polyacrylamide acrylic acid and polyacrylamide acrylonitrile impregnated with inorganic ion exchanger, magneso-silicate, have been synthesized by subjected co-monomers to gamma radiation initiated polymerization at radiation doses 25, 65 and 90 KGy. The structure features of composites were investigated by sequential x-ray fluorescence spectrometer, x-ray diffraction, differential thermal- thermogravimetric analyses and infrared spectroscopy. Formation mechanism for these composites was conducted and the results obtained showed that the polymerization process was carried out in the hydrocarbon chain by addition polymerization whereas impregnation of magneso-silicate into the polymeric composites was carried out by condensation polymerization.
采用沉淀法合成了硅酸镁。用无机离子交换剂镁硅酸盐浸渍聚丙烯酰胺丙烯酸和聚丙烯酰胺丙烯腈,在辐射剂量为25、65和90 KGy的条件下进行聚合反应,合成了聚丙烯酰胺丙烯酸和聚丙烯酰胺丙烯腈。采用序贯x射线荧光光谱仪、x射线衍射仪、差热-热重分析和红外光谱分析研究了复合材料的结构特征。研究了复合材料的形成机理,结果表明,复合材料的聚合过程是在烃链上通过加成聚合进行的,而硅酸镁的浸渍是通过缩聚聚合进行的。
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引用次数: 1
Synthesis of C-glycosides from 1,6-Diamino-4-Phenylpyridine Derivatives 1,6-二氨基-4-苯基吡啶衍生物合成c -糖苷
Pub Date : 2014-01-01 DOI: 10.13189/UJC.2014.020503
A. Amer, A. Ghoneim, Mohamed H.Sherif, W. Farouk
Diamino 3a and 3b derivatives which obtained by Michael reaction were coupled with aldoses in the presence of acetic acid and I2 with stirring at roomtemperature gave 4, 5 and 6 respectively.Acetylation of compound 4 and 5 gave compound 7 and 8 respectively. Coupling of fructose with 3a and 3b in the presence or not of Con HCl gave compound 9 and 11 respectively. Acetylation of compound 9 with acetic anhydride and Pyridine gave compound 10. Some of the synthesized compounds have been screened as antibacterial and antifungal. The structures of the synthesized compounds have been deduced from their elemental analysis and spectral (IR, 1HNMR) data.
将Michael反应得到的二氨基3a和3b衍生物与醛糖在乙酸和I2存在下偶联,在室温搅拌下分别得到4、5和6。化合物4和5乙酰化后分别得到化合物7和8。在Con HCl存在或不存在的情况下,将果糖与3a和3b偶联,分别得到化合物9和11。化合物9与乙酸酐和吡啶乙酰化得到化合物10。合成的部分化合物经筛选具有抗菌和抗真菌作用。通过元素分析和光谱(IR, 1HNMR)数据推断了合成化合物的结构。
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引用次数: 0
Starch sulfuric acid: An alternative, eco-friendly catalyst for Biginelli reaction 淀粉硫酸:一种替代的、环保的比基内利反应催化剂
Pub Date : 2013-12-01 DOI: 10.19261/CJM.2013.08(2).13
R. Rezaei, M. Farjam, Sara Malek, M. Sheikhi
The one-pot multicomponent synthesis of 3,4-dihydropyrimidinone derivativesusingstarch sulfuric acid as an environmentallyfriendly biopolymerbased solid acid catalyst from aldehydes, â-keto esters and urea/thiourea without solvent is described. Compared with classical Biginelli reaction conditions, this new methodhas the advantage of minimizing the cost operational hazards and environmental pollution, good yields, shorter reaction times and simplework-up.
以淀粉硫酸为环境友好型固体酸催化剂,以醛、酮酯和尿素/硫脲为原料,无溶剂一锅多组分合成了3,4-二氢嘧啶衍生物。与传统的Biginelli反应条件相比,该方法具有成本、操作危害和环境污染最小、产率好、反应时间短、处理简单等优点。
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引用次数: 3
Topological descriptors based quantitative structure activity relationship study of aromatic amines 基于拓扑描述符的芳香胺定量构效关系研究
Pub Date : 2008-01-01 DOI: 10.24214/jcbps.a.8.3.39299
P.P.Singh, A. Prajapati
QSAR study of 29 aniline derivatives whose carcinogenic activities are reported in terms of log P has been made. QSAR models have been developed with the help of descriptors,connectivity index,valence connectivity index,shape index,molecularweight,accessibility surface area andmolar refractivity. Thirty-eight models have been found to have high degree of predictive power with regression coefficient above 0.9 and 12models above 0.9597. The combination of descriptors providing the best model is log P,valence connectivity index,shape index and molecular weight.
对29种以log P表示致癌活性的苯胺衍生物进行了QSAR研究。利用描述符、连通性指数、价连通性指数、形状指数、分子量、可及性表面积和摩尔折射率建立了QSAR模型。回归系数在0.9以上的模型有38个,回归系数在0.9597以上的模型有12个。提供最佳模型的描述符组合是log P、价连通性指数、形状指数和分子量。
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引用次数: 0
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Organic Chemistry: An Indian Journal
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