共查询到20条相似文献,搜索用时 359 毫秒
1.
2.
将邻羟苯基引入1,2,3-三唑结构中, 设计合成了10个1-(4-取代苯基)-4-苯基-5-取代-1,2,3-三唑类衍生物. 首先, 以对位取代的芳胺为原料, 经重氮化、叠氮化、闭环和缩合反应制得1-(4-取代苯基)-4-苯基-5-水杨醛亚胺-1,2,3-三唑类衍生物(3a~3e), 再用硼氢化钠还原制得1-(4-取代苯基)-4-苯基-5-(2-羟基苄基)氨基-1,2,3-三唑类衍生物(4a~4e). 目标化合物的结构经核磁、IR及元素分析确认. 抑菌活性测试表明, 当质量浓度为0.1 mg/L时, 除化合物3e和4e外, 所有化合物对白色念球菌的抑菌率均达95%以上, 对大肠杆菌的抑菌率达85%以上, 具有强抑菌活性, 表明该类化合物在抗菌药物开发方面有重要应用价值. 相似文献
3.
4.
以(S)-2-氨基丙醇和氯乙酰氯为起始原料,经酰化和环合反应制得(S)-5-甲基吗啉-3-酮(4); 4经还原制得(S)-3-甲基吗啉(5); 5与4-溴-2-甲基苯甲酸酰化缩合合成了(S)-(4-溴2-甲基苯基)(3-甲基吗啉)-甲酮,总收率57%,其结构经1H NMR 和 13C NMR确证。 相似文献
5.
6.
以糠醛为原料,经氧化、醚化和重结晶制得5-甲氧基-3,4-二溴-2(5H)-呋喃酮(4); 4与哌嗪经Michael加成消除反应制得5-甲氧基-4-哌嗪基-3-溴-2(5H)-呋喃酮(5); 5与取代磺酰氯经磺酰化反应合成了7 个新型的含哌嗪-磺酰胺的2(5H)-呋喃酮类化合物(7a~7g),其结构经1H NMR, 13C NMR, IR和HR-MS表征。初步的生物活性研究(MTT法)表明,7a~7g均能显著抑制人宫颈癌Hela细胞的增殖,其中5-甲氧基-4-(对乙酰氨基苯磺酰基-哌嗪基)-3-溴-2(5H)-呋喃酮(7f)的抑制活性最佳,其IC50为0.03 μM(24 h)。 相似文献
7.
8.
9.
10.
以2-羟基-5-溴苯甲醛为起始原料,经取代,还原和NBS溴化反应制得5-溴-2-(4-氯苯甲氧基)溴甲苯(3);以4-哌啶酮盐酸盐为原料,经保护,还原和缩合反应制得N-烯丙基-2-溴-N-哌啶基苯酰胺(7);3和7经取代反应合成了一个新型的非肽类小分子CCR5拮抗剂——N-烯丙基-2-溴-N-{N-[2-(4-氯苯甲氧基)-5-溴苄基]-4-哌啶基}苯酰胺(8),总产率32.5%,其结构经1H NMR,13C NMR,IR和ESI-MS表征。用GTPγS法测试了8的生物结合性。结果表明:8的生物结合性与TD0232接近,其IC50为(8.12±0.3)nmol·L-1。 相似文献
11.
12.
13.
14.
15.
16.
H J Reeuwijk H Lingeman U R Tjaden E A de Bruijn H J Keizer J van der Greef 《Journal of chromatography. A》1988,428(1):93-102
(E)-5-(2-Bromovinyl)-2'-deoxyuridine is an antiviral drug that is experimentally used for modulation of the antitumour effect of fluoropyrimidines, such as ftorafur and 5-fluorouracil. The isolation of the analyte, in the presence of 5-fluorouracil, from the matrix is performed either by means of a simple protein precipitation (plasma) or by means of a liquid-liquid extraction with ethyl acetate (urine). Following pretreatment, the analyte is analysed by reversed-phase chromatography and quantified by absorbance detection at 307 nm. The minimum detectable concentration in plasma and urine samples is ca. 6 ng/ml. The recovery after deproteination of plasma samples is 75%, while after liquid-liquid extraction of urine the recovery amounts 92%. The degree of protein binding of the analyte, measured by ultrafiltration, is found to be 97%. These data allow the bioanalysis of (E)-5-(2-bromovinyl)-2'-deoxyuridine for pharmacokinetic studies. 相似文献
17.
Yousef TA Abu El-Reash GM Rakha TH El-Ayaan U 《Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy》2011,83(1):271-278
Manganese(II), iron(II), cobalt(II), nickel(II), copper(II), and chromium(III) complexes of (E)-2-(2-(2-hydroxybenzylidene)hydrazinyl)-2-oxo-N-phenylacetamide were synthesized and characterized by elemental and thermal (TG and DTA) analyses, IR, UV-vis and (1)H NMR spectra as well as magnetic moment. Mononuclear complexes are obtained with 1:1 molar ratio except [Mn(HOS)(2)(H(2)O)(2)] and [Co(OS)(2)](H(2)O)(2) complexes which are obtained with 1:2 molar ratios. The IR spectra of ligand and metal complexes reveal various modes of chelation. The ligand behaves as a monobasic bidentate one and coordination occurs via the enolic oxygen atom and azomethine nitrogen atom. The ligand behaves also as a monobasic tridentate one and coordination occurs through the carbonyl oxygen atom, azomethine nitrogen atom and the hydroxyl oxygen. Moreover, the ligand behaves as a dibasic tridentate and coordination occurs via the enolic oxygen, azomethine nitrogen and the hydroxyl oxygen atoms. The electronic spectra and magnetic moment measurements reveal that all complexes possess octahedral geometry except the copper complexes possesses a square planar geometry. From the modeling studies, the bond length, bond angle, HOMO, LUMO and dipole moment had been calculated to confirm the geometry of the ligands and their investigated complexes. The thermal studies showed the type of water molecules involved in metal complexes as well as the thermal decomposition of some metal complexes. The protonation constant of the ligand and the stability constant of metal complexes were determined pH-metrically in 50% (v/v) dioxane-water mixture at 298 K and found to be consistent with Irving-Williams order. Moreover, the minimal inhibitory concentration (MIC) of these compounds against Staphylococcus aureus, Escherechia coli and Candida albicans were determined. 相似文献
18.
2-(芳磺酰基)-1-(2-噻吩基)乙酮的合成丁言斌樊爱龙张正*(南京大学化学系南京210093)关键词氯噻吩基乙酮,芳磺酰基噻吩基乙酮,合成,相转移催化1996-08-12收稿,1997-01-13修回砜类化合物不仅是有机合成的有用中间体[1],而... 相似文献
19.
Optically active (S)-2-(2-methylbutyl)thiophene was obtained by different procedures. Among them, the cross-coupling reaction between 2-methylbutylmagnesium chloride and 2-chlorothio-phene proved to be the most efficient one. Compound 1 was thus obtained in satisfactory yield and rather high optical purity (82%). 相似文献
20.
Quantum-chemical calculations (B3LYP/6-31G*) predict the formation of intramolecular hydrogen bond (IMHB) in the monoprotonated
Z-isomer of 1-(2-pyridyl)-2-(2-quinolyl)ethylene (2P2Q), with this bond stabilizing the isomer relative to its E-counterpart. An experimentally observed increase in the quantum yield of trans-cis photoisomerization (φtc) by more than an order of magnitude (from 0.033 to 0.42 in acetonitrile) on passing from the neutral to the monoprotonated
form of 2P2Q can be associated with IMHB, which manifested itself in the spectral properties of the Z-isomer. The IMHB breaks in the diprotonated form, and the value of φtc decreases back to the initial value. In addition to the photoisomerization, the photoreduction and photoaddition reactions
of solvent molecules have been observed in an ethanol solution of 2P2Q. 相似文献