共查询到20条相似文献,搜索用时 31 毫秒
1.
Bennett NJ Elliott MC Hewitt NL Kariuki BM Morton CA Raw SA Tomasi S 《Organic & biomolecular chemistry》2012,10(19):3859-3865
The deprotonation and alkylation of 1-methylcyclohexa-2,5-diene-1-carboxylic acid has been investigated under a range of conditions. In all cases, the formation of compounds 14 was found to be completely stereoselective, although compound 14c was formed as an impurity when alkyl iodides were used as electrophiles, and doubly-alkylated compounds 17 were formed in some cases when alkyl bromides were used. 相似文献
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E. G. Mamedbeili I. A. Dzhafarov K. A. Kochetkov Kh. I. Gasanov S. T. Alieva 《Russian Journal of Organic Chemistry》2010,46(2):177-179
Synthesis was performed of new aminomethoxy derivatives of 1-propylsulfanyl hexane by Mannich condensation of 1-propanethiol,
secondary amines, and formaldehyde. The structure of compounds synthesized was established by elemental analysis, mass spectrometry,
IR and 1H NMR spectroscopy. Some compounds obtained were tested as antimicrobial additives to lubricating oils, and also as antiseptics
against bacteria and fungi. It was established that these compounds are more efficient antimicrobial substances than the preparations
currently used. 相似文献
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The metabolites of 1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-1H-b enzimidazole difumarate (KG-2413), which has a potent H1-antihistaminic activity, were predicted on the basis of metabolic studies of related compounds and were synthesized to aid in identification of the actual metabolites and for examination of their antihistaminic activity. Among the twelve compounds prepared, nine compounds were actually found as the metabolites of KG-2413 in rat urine. The antihistaminic activities of these metabolites were found to be lower than that of KG-2413. 相似文献
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I. A. Dzhafarov E. G. Mamedbeili V. S. Gasanov Kh. I. Gasanov 《Russian Journal of Applied Chemistry》2009,82(4):693-695
The possibility of synthesizing new methyleneoxyamino derivatives of 1-butylthioheptane was investigated. The structure of the synthesized compounds was proved by elemental analysis and IR and 1H NMR spectroscopy. Some representatives of the synthesized compounds were tested as antimicrobial lubricant additives, and also as antiseptic materials against bacteria and funguses. 相似文献
6.
A. S. Kulikov M. A. Epishina L. V. Batog V. Yu. Rozhkov N. N. Makhova L. D. Konyushkin M. N. Semenova V. V. Semenov 《Russian Chemical Bulletin》2013,62(3):836-843
A method of 3-amino-4-[5-aryl(heteroaryl)-1H-1,2,3-triazol-1-yl)]furazan synthesis was optimized. Condensation of these compounds with 2,5-dimethoxytetrahydrofuran resulted in a series of previously unknown 4-[5-aryl(heteroaryl)-1H-1,2,3-triazol-1-yl)]-3-(pyrrol-1-yl)furazans. All target compounds were evaluated for both antimitotic microtubule destabilizing effect in a phenotypic sea urchin embryo assay and cytotoxicity in a panel of 60 human cancer cell lines. Pyrrolyl derivatives of triazolylfurazans were determined as antiproliferative compounds. The most potent microtubule targeting compounds 7a and 7e are of interest for further trials as antineoplastic agents. 相似文献
7.
A series of 1-methyl-1H-benzimidazole-based compounds, 2-(4?-alkoxy-1,1?-biphenyl-4-yl)-1-methyl- 1H-1,3-benzimidazole derivatives (nPPMx-M) with terminal hydrogen, methyl and nitro moieties (coded as nPPMH-M, nPPMM-M and nPPMN-M, respectively), were prepared and their structures were characterised. The compounds display enantiotropic smectic mesophases for hydrogen and methyl terminated compounds (nPPMH-M and nPPMM-M), and enantiotropic nematic mesophases for nitro terminated compounds (nPPMN-M) with short alkoxy chain below than 10 carbon atoms, where the mesophase ranges are 24–72°C and 74–104°C on heating and cooling processes for nPPMH-M, 90–119°C and 110–135°C for nPPMM-M, and 102–129°C and 113–207°C for nPPMN-M, respectively. It is noted that the compounds nPPMx-M exhibit much lower melting points and much wider mesophase range both in heating and cooling than non-1-methyl substituted analogs, which are ascribed to the disruption of hydrogen bonding among the molecules caused by methyl substitution at 1-position of benzimidazole. Meanwhile, among the compounds nPPMx-M, much wider mesophase ranges are obtained for nPPMM-M and nPPMN-M, indicating a much high mesophase stability for the compounds bearing terminal moiety (CH3 and NO2). 相似文献
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通过二溴化物与唑酮1[R=(CH3)3C]或α-三唑基苯乙酮1(R=Ar)的亲核取代反应,合成了新型的环状三唑类化合物3和4,经元素分析,1HNMR,IR,EI-MS和X射线衍射等方法确证其结构,讨论了反应过程.生物活性测试发现大部分化合物具有很好的杀菌活性,尤其对小麦锈病具有较强的抑制作用. 相似文献
10.
1-Thiohydroxypyrene(1) and its two intermediates, 1-pyrenyl-O-thiocarbamate(2) and 1-pyrenyl-S-thio- carbamate(3), were synthesized using 1-hydroxypyrene as the starting material. The key synthetic step is Newman-Kwart rearrangement. The results indicate that the Newman-Kwart rearrangement is more effective in suitable solvent than conventional method based on pure organic compound. The structures of compounds 1―3 were characterized by FTIR, NMR, GC-MS and elementary analysis. The crystal structures of two new compounds(2 and 3) were determined by single crystal X-ray diffraction analysis. The whole synthetic process is simple, mild and with high yield. 相似文献
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E. H. Mamedbeyli I. A. Jafarov G. M. Talybov M. A. Mirzoeva K. O. Iskenderova A. N. Hajizade 《Russian Journal of General Chemistry》2017,87(4):713-716
New aminomethoxy derivatives of 1-(butylsulfanyl)pentane have been synthesized. The structure of the synthesized compounds was studied by elemental analysis, IR and 1Н NMR spectroscopy, and mass spectrometry. Some specimens of the synthesized compounds were tested as antimicrobial additives to lubricant oil, and as aseptic compounds against bacteria and fungi. 相似文献
14.
ZHOU Yun-yun LI Yu-xin LI Yi-ming YANG Xiao-ping MAO Ming-zhen LI Zheng-ming 《高等学校化学研究》2013,29(2):249-255
Carbohydrates, with broad-spectrum structures and biological functions, are key organic compounds in nature, along with nucleic acids and proteins. As part of our ongoing efforts to develop a new class of pesticides with novel mechanism of action, a series of novel N-glycosyl-1-pyridyl-1H-pyrazole-5-carboxamide was designed and synthesized via the reactions of glycosyl methanamides and pyridyl-pyrazole acid. The compounds were characterized by 1H NMR and 13C NMR. The bioassay results indicate that some of these compounds exhibit moderate insecticidal activities and assessed as potential inhibitors of calcium channels. The modulation of voltage-gated calcium channels by compounds 4a and 5a in the central neurons isolated from the third instar larvae of Spodoptera exigua was studied by whole-cell patch-clamp technique. In addition, compound 5a inhibits the recorded calcium currents reversible on washout. Experimental results also indicate that compound 5a did not release stored calcium from the Endoplasmic Reticulum. The present work demonstrates that N-glycosyl-1-pyridyl-1H-pyrazole-5-carboxamides cannot be used as possible inhibitors of calcium channels for developing novel pesticides. 相似文献
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Choji Kashima Tadakuni Tajima And Yoshimori Omote 《Journal of heterocyclic chemistry》1984,21(1):133-137
2-Alken-1-ones, 3,3-di-(1-azolyl)-2-alken-1-ones and related compounds were prepared by two methods. These compounds were found to be the useful precursors for acylketene derivatives such as ketene dithioacetals and diaminals by treatment with various nucleophiles. 相似文献
17.
Malmström J Jonsson M Cotgreave IA Hammarström L Sjödin M Engman L 《Journal of the American Chemical Society》2001,123(15):3434-3440
A novel synthesis of 2,3-dihydrobenzo[b]thiophene-5-ol based on intramolecular homolytic substitution on sulfur was reported. The "antioxidant profile" of the series of 2,3-dihydrobenzo[b]furan-5-ol (2a) its 1-thio (2b), 1-seleno (2c) and 1-telluro (2d) analogues was determined by studies of redox properties, the capacity to inhibit stimulated lipid peroxidation, the reactivity toward tert-butoxyl radicals, the ability to catalyze decomposition of hydrogen peroxide in the presence of glutathione, and the inhibiting effect on stimulated peroxidation in liver microsomes. The one-electron reduction potentials of the aroxyl radicals corresponding to compounds 2a-2d, E degrees (ArO(*)/ArO(-)) were 0.49, 0.49, 0.49, and 0.52 V vs NHE, respectively, as determined by pulse radiolysis. With increasing chalcogen substitution the compounds become slightly more acidic (pK(a) = 10.6, 10.0, 9.9, and 9.5, respectively, for compounds 2a-2d). By using Hess' law, the homolytic O-H bond dissociation enthalpies of compounds 2a-2d (340, 337, 336, and 337 kJ mol(-)(1), respectively) were calculated. The reduction potentials for the proton coupled oxidation of compounds 2a-2d (ArOH --> ArO(*) + H(+)) as determined by cyclic voltammetry in acetonitrile were 1.35 (irreversible), 1.35 (quasireversible) 1.13 (reversible), and 0.74 (reversible) V vs NHE, respectively. As judged by the inhibited rates of peroxidation, R(inh), in a water/chlorobenzene two-phase lipid peroxidation system containing N-acetylcysteine as a thiol-reducing agent in the aqueous phase, the antioxidant capacity increases (2d > 2c = 2b > 2a) as one traverses the group of chalcogens. Whereas the times of inhibition, T(inh), were slightly reduced for the oxygen (2a) and sulfur (2b) derivatives in the absence of the thiol-reducing agent, they were drastically reduced for the selenium (2c) and tellurium (2d) derivatives. This seems to indicate that the organochalcogen compounds are continuously regenerated at the lipid aqueous interphase and that regeneration is much more efficient for the selenium and tellurium compounds. The absolute rate constants for the oxidation of compounds 2a-2b by the tert-butoxyl radical in acetonitrile/di-tert-butyl peroxide (10/1) were the same-2 x 10(8) M(-)(1) s(-)(1). Whereas the oxygen, sulfur, and selenium derivatives 2a-2c were essentially void of any glutathione peroxidase-like activity, the organotellurium compound 2d accelerated the initial reduction of hydrogen peroxide, tert-butyl hydroperoxide, and cumene hydroperoxide in the presence of glutathione 100, 333, and 213 times, respectively, as compared to the spontaneous reaction. Compounds 2a-2d were assessed for their capacity to inhibit lipid peroxidation in liver microsomes stimulated by Fe(II)/ADP/ascorbate. Whereas the oxygen, sulfur, and selenium compounds showed weak inhibiting activity (IC(50) values of approximately 250, 25, and 13 microM, respectively), the organotellurium compound 2d was a potent inhibitor with an IC(50) value of 0.13 microM. 相似文献
18.
Sangma C Chuakheaw D Jongkon N Saenbandit K Nunrium P Uthayopas P Hannongbua S 《Combinatorial chemistry & high throughput screening》2005,8(5):417-429
The virtual screening approach for docking small molecules into a known protein structure is a powerful tool for drug design. In this work, a combined docking and neural network approach, using a self-organizing map, has been developed and applied to screen anti-HIV-1 inhibitors for two targets, HIV-1 RT and HIV-1 PR, from active compounds available in the Thai Medicinal Plants Database. Based on nevirapine and calanolide A as reference structures in the HIV-1 RT binding site and XK-263 in the HIV-1 PR binding site, 2,684 compounds in the database were docked into the target enzymes. Self-organizing maps were then generated with respect to three types of pharmacophoric groups. The map of the reference structures were then superimposed on the feature maps of all screened compounds. Only the structures having similar features to the reference compounds were accepted. By using the SOMs, the number of candidates for HIV-1 RT was reduced to six and nine compounds consistent with nevirapine and calanolide A, respectively, as references. For the HIV-1 PR target, there are 135 screened compounds showed good agreement with the XK-263 feature map. These screened compounds will be further tested for their HIV-1 inhibitory affinities. The obtained results indicate that this combined method is clearly helpful to perform the successive screening and to reduce the analyzing step from AutoDock and scoring procedure. 相似文献
19.
Ji-Wang Chem Hua-Mei Lin Fong-Chi Cheng Jir-Chun Lo Nan-Yi Lai Chai-Lin Kao Cyril O. Usifoh 《中国化学会会志》1998,45(6):805-810
In the course of our investigations on the development of cardiovascular agents, 3-butyl-2-[2′-(2H-tetrazol-5-yl)bipheny]-4-yl]methyl-2H-1, 2, 4-benzothiadiazine 1, 1-dioxide ( 2 ) was considered as a potential angiotensin II antagonist on the basis of bioisosteric replacement of the quinazoline ring of compound 1 with a 1, 2, 4-benzothiadiazine 1, 1-dioxide ring system. Alkylation of 6 with 4 afforded 7 and 8 in 24% and 28% yields, respectively. An attempt to remove the trityl group of compounds 7 and 8 under acidic condition gave the ring opened products 9 and 11 in 28% and 36% yields, respectively. However, compounds 2 and 10 were obtained in 46% and 85% yields when compounds 7 and 8 were refluxed in methanol. Preliminary assays of compounds 9 and 11 against angiotensin II receptors revealed weak activity with IC50 values of 3.6 μM and 5.4 μM, respectively. Compound 10 (IC50 = 87 nM) exhibited stronger binding affinity than compound 2 (IC50 = 750 nM). 相似文献
20.
用过氧化氢氧化烯烃得到顺式邻环己二醇,继而和对甲苯磺酰氯反应得到两种1-取代-顺式-1,2-环己二醇单磺酸酯.以溴酚兰作指示剂,用作者自己的方法定量测定了它们在聚乙二醇膜层中的酸解性能.结果表明,在光产酸剂所产酸作用下,在加热条件下这些化合物发生分解并产酸.这两个磺酸酯的储存稳定性不是很好,在极性溶剂作用下易分解,限制了它们在化学增幅型成像材料中的应用. 相似文献