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Omer A. Akrawi Gergő Z. Nagy Tamás Patonay Alexander Villinger Peter Langer 《Tetrahedron letters》2012,53(26):3206-3209
Suzuki–Miyaura reactions of 4-trifluoromethylsulfonyloxy-6-bromocoumarin provide a convenient access to arylated coumarins. The reactions proceed with excellent chemoselectivity in favour of position 4. 相似文献
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Gergő Tóth Réka Mohácsi Ákos Rácz Aura Rusu Péter Horváth Lajos Szente Szabolcs Béni Béla Noszál 《Journal of inclusion phenomena and macrocyclic chemistry》2013,77(1-4):291-300
The enantiomer-specific characterization of ofloxacin–cyclodextrin complexes was carried out by a set of complementary analytical techniques. The apparent stability constants of the ofloxacin enantiomers with 20 different cyclodextrins at two different pH values were determined to achieve good resolution capillary electrophoresis enantioseparation either to establish enantioselective drug analysis assay, or to interpret and design improved host–guest interactions at the molecular level. The cyclodextrins studied differed in the nature of substituents, degree of substitution (DS), charge and purity, allowing a systematic test of these properties on the complexation. The seven-membered beta-cyclodextrin and its derivatives were found to be the most suitable hosts. Highest stability and best enantioseparation were observed for the carboxymethylated-beta-cyclodextrin (DS ~ 3.5). The effect of substitution pattern (SP) was investigated by molecular modeling, verifying that SP greatly affects the complex stability. Induced circular dichroism was observed and found especially significant on carboxymethylated-beta-cyclodextrin. The complex stoichiometry and the geometry of the inclusion complexes were determined by 1H NMR spectroscopy, including 2D ROESY techniques. Irrespective of the kind of cyclodextrin, the complexation ratio was found to be 1:1. The alfa-cyclodextrin cavity can accommodate the oxazine ring only, whereas the whole tricyclic moiety can enter the beta- and gamma-cyclodextrin cavities. These equilibrium and structural information offer molecular basis for improved drug formulation. 相似文献
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Zoltán-István Szabó Réka Gál Zsolt Gáll Szende Vancea Emőke Rédai Ibolya Fülöp Emese Sipos Gabriella Donáth-Nagy Béla Noszál Gergő Tóth 《Journal of inclusion phenomena and macrocyclic chemistry》2017,88(1-2):43-52
Rufinamide (RUF) was characterized in terms of cyclodextrin (CD) complexation in order to improve its aqueous solubility. Binary systems of RUF with three CDs—β-cyclodextrin (β-CD), randomly methylated-β-cyclodextrin (RAMEB) and sulfobutylether-β-cyclodextrin (SBE-β-CD)—were characterized with a wide variety of analytical techniques. Liquid state characterization was carried out by complementary techniques such as nuclear magnetic resonance spectroscopy (NMR), capillary electrophoresis (CE), mass spectrometry (MS) and phase solubility studies. The latter revealed that the stability of the complexes decreased in the order of RAMEB?>?β-CD?>?SBE-β-CD. AL-type diagrams were obtained in all cases, characteristic of 1:1 stoichiometry, with a maximum of over 15-fold increase in RUF solubility, when complexed with RAMEB. NMR Job plot and MS studies confirmed phase solubility results, regarding the binding stoichiometry. 1H NMR and 2D ROESY investigations revealed the inclusion of the triazole moiety of RUF, confirmed by molecular modeling. Solid state complexation in 1:1 molar ratio was carried out by kneading method and investigated by differential scanning calorimetry (DSC) and infrared spectroscopy (IR). Comparative dissolution studies indicated an over two-fold improvement in dissolution efficacy of the kneaded products, when compared to the pure drug. Results of the present study might pave the way for a drug formulation with improved bioavailability. 相似文献
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The set \({{\mathrm{Quo}}}(\mathbf {A})\) of compatible quasiorders (reflexive and transitive relations) of an algebra \(\mathbf {A}\) forms a lattice under inclusion, and the lattice \({{\mathrm{Con}}}(\mathbf {A})\) of congruences of \(\mathbf {A}\) is a sublattice of \({{\mathrm{Quo}}}(\mathbf {A})\). We study how the shape of congruence lattices of algebras in a variety determine the shape of quasiorder lattices in the variety. In particular, we prove that a locally finite variety is congruence distributive [modular] if and only if it is quasiorder distributive [modular]. We show that the same property does not hold for meet semi-distributivity. From tame congruence theory we know that locally finite congruence meet semi-distributive varieties are characterized by having no sublattice of congruence lattices isomorphic to the lattice \(\mathbf {M}_3\). We prove that the same holds for quasiorder lattices of finite algebras in arbitrary congruence meet semi-distributive varieties, but does not hold for quasiorder lattices of infinite algebras even in the variety of semilattices. 相似文献
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Order - In this paper, we investigate the class of lattices representable with posets satisfying the DCC condition. We describe a way to decide whether a finite lattice is in this class. We also... 相似文献