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研究了3种环糊精对奥美沙坦酯药物的增溶效果。建立了高效液相色谱法测定环糊精溶液中奥美沙坦酯药物含量的方法,利用相溶解度法测定了奥美沙坦酯在不同浓度的β-环糊精(β-CD)、甲基-β-环糊精(M-β-CD)、羟丙基-β-环糊精(HP-β-CD)溶液中的溶解度,并绘制了相溶解度曲线。在0~15 mmol/L环糊精浓度范围内,奥美沙坦酯的溶解度随3种环糊精浓度的增加而线性增加,相溶解度曲线呈AL型,奥美沙坦酯与3种环糊精均是1:1的比例包合;3种环糊精对奥美沙坦酯均有显著的增溶作用且羟丙基-β-环糊精的增溶效果最佳,其次为甲基-β-环糊精和β-环糊精。 相似文献
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分别以2种天然环糊精(β、γ-环糊精)、2种常用的电中性环糊精衍生物(羟丙基-β-环糊精、二甲基-β-环糊精)和3种新型荷电环糊精衍生物(高取代磺酸基α、β、γ-环糊精)作为毛细管区带电泳手性添加剂,研究了环糊精的类型对6种手性药物对映体分离的影响.2种天然环糊精对所研究的手性药物均无手性识别能力,而环糊精经过衍生化后手性识别能力得到了很大的提髙,尤其是高取代磺酸基β-环糊精使6种手性药物均得到了基线分离.还考察了缓冲溶液的pH值和有机添加剂对手性分离的影响. 相似文献
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环糊精衍生物在液相有机合成中的应用 总被引:1,自引:0,他引:1
综述了环糊精(包括α-环糊精、β-环糊精和y-环糊精)衍生物在液相有机合成中的应用,主要包括其作为人工合成酶、超分子光学手性源、亲偶极体和微通道反应器在氧化、水解、还原、光催化异构化、1,3-偶极环加成等反应中的应用.其中环糊精衍生物作为人工合成酶应用最广,该催化剂中起催化作用的为环糊精衍生物的修饰基团.与环糊精母体相比,修饰基团的引入增加了环糊精分子中官能团的种类和数量,拓展了环糊精在液相有机合成中的应用,并提高了催化反应的催化活性和选择性. 相似文献
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环糊精是一类由吡喃葡萄糖单元构成的大环分子,能够通过包结作用与多种小分子、金属离子以及聚合物形成主-客体包结物,从而实现对客体分子理化性能的调控,被广泛用于制药、食品、化学、色谱、催化、生物技术、农业、化妆品、卫生、医学、纺织和环境等领域.然而,环糊精分子在众多应用领域不易操控,通过化学交联制备环糊精聚合物,形成以环糊精为主体的聚合物,则有望实现环糊精与交联基团的"集成"和"协同"作用,不但能有效解决环糊精分子的操控问题,而且能够赋予环糊精单分子所不具有的独特功能和理化性质,因此环糊精聚合物的设计合成及其应用吸引了广泛的研究兴趣.本综述介绍了环糊精聚合物领域的研究近况,对环糊精聚合物的种类按结构与性质进行了分类,系统介绍了各类环糊精聚合物的制备方法,重点介绍了近五年环糊精聚合物取得的新突破,并详细论述了各类环糊精聚合物在生物医药中的应用和其他领域的代表性应用,最后对环糊精聚合物作了简要总结和展望. 相似文献
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毛细管电泳环糊精添加剂拆分特布他林对映体的立体选择性研究 总被引:2,自引:0,他引:2
分别测定了毛细管区带电泳环糊精手性拆分体系中α,β-环糊精和二甲基、三甲基、羟丙基-β-环糊精与药物对映体特布他林形成包结络合物的稳定常数以及手性拆分过程的热力学函数的变化。数据分析表明,环糊精稳定常数的大小反映了环糊精空腔与分离对象之间的匹配程度。环糊精稳定常数的相对值反映了手性拆分体系的分离能力。两对映体与环糊精所形成包结络合物的Δ(ΔH)和Δ(ΔS)分别反映了手性拆分过程中立体作用与构象匹配的差异。与甲基化β-环糊精相比,羟丙基-β-环糊精和β-环糊精提供的氢键作用在手性拆分中起着重要作用。 相似文献
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利用质谱仪,使用电喷雾离子源,分别研究了以α-环糊精、β-环糊精和产环糊精作为手性拆分剂对手性药物甲基麻黄碱的手性识别效应.实验结果表明,3种环糊精对甲基麻黄碱对映体均有较强的手性识别效应,Rchiral分别为2.43、3.51、4.52.研究了电压的变化对α-环糊精、β-环糊精和γ-环糊精的手性识别的影响,研究发现,在不同的电压下,这3种环糊精对甲基麻黄碱均有手性识别能力. 相似文献
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Abstract The structure of the host compound trans-9,10-dihydroxy-9,10-di-p-tolyl-9,10-dihydroanthracene and those of its inclusion compounds with acetone, diethyl ether and pyridine have been elucidated. The non-porous α-phase of the host has a structure in which the molecules are packed in layers parallel to the (100) plane, but exhibit no intermolecular hydrogen bonding. The host:guest stoichiometry of each inclusion compound is 1:2, and the structures are each stabilised by O-H…O or O-H…N hydrogen bonds between host and guest. The thermal decompositions of the acetone and diethyl ether compounds are characterised by single endotherms of the guest-release reaction, but the pyridine inclusion compound has a more complex decomposition, characteristic of similar pyridine inclusion compounds. 相似文献
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Roger Bishop Donald C. Craig Ian G. Dance Sungho Kim Md. Aminul I. Mallick Kim C. Pich 《Supramolecular chemistry》2013,25(2):171-178
Abstract In order to be able to predict and then synthesize new lattice inclusion compounds with the helical tubuland diol host structure, the hydrogen bonding modes of a range of bicyclic and tricyclic diols have been studied using X-ray crystallography. Several distinct types of lattice structure have been recognized. Steric factors play a major role in determining which of these is produced in a given case. Establishment of a series of structural rules provides a window of opportunity for duplication of the helical tubuland host lattice by deliberate design and synthesis. New inclusion compounds resulting from this approach are presented. 相似文献
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The cyclodextrins(CDs) are a class of cyclic oligosaccharides made up of six(a), seven(a)or more [a-(1,4)-linked] D-glucopyranose units, and shaped like truncated cones with primary and secondary hydroxyl groups crowning the narrower rim and wider rim respectively. As they have a hydrophobic cavity of appropriate dimension, they can bind with various guest moleculars, such as hydrocarbon, cyclohexane, aromatic compounds, to form inclusion complexes. The cyclodextins inclusion complexation has been considered an ideal model mimicking the enzyme-substrate interaction and a lot of effect has been devoted to it. In this paper, we report our investigation on the inclusion complexation behavior of a-cyclodextrin(a-CD) with diphenyl compounds in order to further explore the molecular recongnition mechanism of 2:1 inclusion complexation of a-CD with aromatic compounds.Figure 1: Possible structures of the inclusion compounds.The inclusion complexation behavior of a-CD with sym-diphenyl-urea, sym-diphenyl-thiourea and diphenyl kotone as respective guest moleclars was studied by ultraviolet spectrometric titrations.The absorption spectral changes observed for the compounds in the absence and presence of a-CD are used to draw the corresponding Benesi-Hildebrand plots and caculate the complex stability constant value (Ks) for the inclusion compounds.The 2:1 inclusion complexations show higher binding constants by cooperative binding of one guest molecular in the closely two hydrophobic cyclodextrin cavites as compared with 1:1 inclusion complexations.The highest value observed for sym-diphenyl-urea could be due to the formation of a hydrogen bond between the carbonyl group and the hydrogen in the hydroxyl group of CD and this is not possible with sym-tiphenyl-thiourea. The lowest value observed for diphenyl kotone indicate the hydrophobic interaction is one of the binding force of cyclodextrin inclusion complex. 相似文献
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Mieczysław Maciejewski Andrzej Gwizdowski Piotr Pęczak Alicja Pietrzak 《高分子科学杂志,A辑:纯化学与应用化学》2013,50(1):87-109
The investigations of the synthesis of polyrotaxanes by the radical polymerization of monomers (vinylidene chloride, methyl acrylate, styrene, and methacrylonitrile) in DMF in the presence of β-cyclodextrin have been carried out. The possibility of formation β-cyclodextrin inclusion compounds with some vinyl monomers or some other organic substances in DMF solution has been established. We assume that the inclusion in presence of the solvent is related to the unusual phenomenon of β-cyclodextrin crystallization in hot DMF solutions. The polymerization of vinyl monomers in DMF solution at increased temperatures in the presence of β-cyclodextrin leads to compounds containing a great amount of cyclic compounds (up to 80%). Similar results have been obtained for monomers introduced as previously prepared adducts with β-cyclodextrin. Stable compounds of polymer and β-cyclodextrin have been obtained in the case of vinylidene chloride. The lack of carbohydrate moieties in the product obtained by polymerization of vinylidene chloride in the presence of linear dextrin suggest the inclusion character of the linkage between polymer and β-cyclodextrin molecules. The structure of a topological compound of polyrotaxane type is most feasible after dehydrochlorination. 相似文献
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A series of 4-arylidenamino-5-phenyl-4H-1,2,4-triazole-3-thiols have been synthesised and their inclusion complexes have been prepared with β-cyclodextrin. The compounds and their inclusion complexes have been characterised by studying their physical and spectral properties. The thermodynamic stability constant and free energy of activation have been determined to know the stability of inclusion complexes. Finally, the compounds and their inclusion complexes are screened for antibacterial, antioxidant and anthelmintic activities. It is found that inclusion complexes of the newly synthesised compounds have appreciable stability and inclusion complex formation increases the antibacterial, antioxidant and anthelmintic activities significantly as compared to naked compound. 相似文献
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Inclusion compounds of gossypol with a number of acetic acid esters have been obtained and have been identified by derivatography and NMR spectroscopy. An x-ray structural investigation of the structures of crystalline complexes of gossypol with ethyl acetate and butyl acetate has shown that these complexes are isostructural semiclathrates. On the basis of the structures of these two semiclathrates of gossypol, it has been concluded that esters and ketone with chain lengths of from five to seven atoms form inclusion compounds isomorphous with the semiclathrates of ethyl and butyl acetates. If the chain length is shorter or longer than that given, inclusion compounds with a different crystal structure are formed.A. S. Sadykov Institute of Bioorganic Chemistry, Uzbek SSR Academy of Sciences, Tashkent. Translated from Khimiya Prirodnykh Soedinenii, No. 5, pp. 669–675, September–October, 1988. 相似文献
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Ziganshin MA Yakimov AV Safina GD Solovieva SE Antipin IS Gorbatchuk VV 《Organic & biomolecular chemistry》2007,5(9):1472-1478
The effect of macrocycle size on the structure-property relationships was studied for inclusion compounds of tert-butylcalix[n]arenes (n=4,5) with volatile organic guests having various molecular size and group composition. Vapor-sorption isotherms, guest-inclusion stoichiometry and Gibbs energy, thermostability parameters and decomposition enthalpies were determined for host-guest compounds (clathrates) obtained using saturation of solid calixarene powder with guest vapor. The increase of the host macrocycle in the studied calixarene pair changes the observed structure-property relationship from the guest-binding selectivity mostly seen in inclusion Gibbs energy to the high sensitivity for guest structure in inclusion stoichiometry. The host with the larger macrocycle has more clathrates with stepwise formation and decomposition. Specific types of guest binding with solid hosts are discussed. 相似文献
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药物研发的过程中,越来越多的化合物存在溶解性低的问题,因此提高药物溶解度是目前迫切需要解决的问题.环糊精、杯芳烃、葫芦脲等大环化合物可以通过主客体作用形成包合物从而增加难溶性药物的水溶性.本文介绍了几种大环化合物在药物增溶领域的应用.首先,基于大环化合物化学结构和空腔属性的差异,列举了它们可增溶药物的种类和范围;其次,... 相似文献
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Guest-free guanidinium organomonosulfonates (GMS) and their inclusion compounds display a variety of lamellar crystalline architectures distinguished by different "up-down" projections of the organomonosulfonate residues on either side of a two-dimensional (2D) hydrogen-bonding network of complementary guanidinium ions (G) and sulfonate moieties (S), the so-called GS sheet. Using a combinatorial library of 24 GMS hosts and 26 guest molecules, a total of 304 inclusion compounds out of a possible 624 possible host-guest combinations were realized, revealing a remarkable capacity of the GMS hosts to form inclusion compounds despite the facile formation of the corresponding guest-free compounds and the absence of "predestined" inclusion cavities like those in related guanidinium organodisulfonate host frameworks. The GS sheets in the inclusion compounds behave as "molecular jaws" in which organomonosulfonate groups projecting from opposing sheets clamp down on the guest molecules, forming ordered interdigitated arrays of the host organic groups and guests. Both the guest-free and inclusion compounds display a variety of architectures that reveal the structural integrity of two-dimensional GS sheet and the unique ability of these hosts to conform to the steric demands of the organic guests. Certain GMS host-guest combinations prompt formation of tubular inclusion compounds in which the GS sheet curls into cylinders with retention of the 2D GS network. The cylinders assemble into hexagonal arrays through interdigitation of the organosulfonate residues that project from their outer surfaces, crystallizing in high-symmetry trigonal or hexagonal space groups. This unique example of network curvature and structural isomerism between lamellar and cylindrical structures, with retention of supramolecular connectivity, is reminiscent of the phase behavior observed in surfactant microstructures and block copolymers. The large number of host-guest combinations explored here permits grouping of the inclusion compound architectures according to the shape of the guests and the relative volumes of the organomonosulfonate groups, enabling more reliable structure prediction for this class of compounds than for molecular crystals in general. 相似文献