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101.
Giuliana Righi Giorgio Scotti Francesco Caruso Miriam Rossi Francesco Mecozzi Roberto Antonioletti Romina Pelagalli 《Tetrahedron》2013
The Lewis acid-catalyzed regioselective azidolysis of 2,3-three membered heterocyclic amines has been investigated. The results obtained demonstrated that using TMSN3 as a source of azide, the appropriate choice of Lewis acid allowed to obtain different regio- and stereocontrolled precursors of aminoalcoholic and triaminic sequences. Considering the occurrence of these moieties in the structure of many biologically active compounds, the present methodologies could represent a powerful tool in organic synthesis for the preparation of interesting molecules. 相似文献
102.
Emiliano Manzo Giuliana D’IppolitoDario Pagano Francesco TintoAngelo Fontana 《Tetrahedron letters》2014
Fluorescent galactolipid analogues (1, 1a, and 2) have been synthesized with a pyrene group attached to the amino-terminal of a hexanoyl chain bound to an otherwise normal galactolipid structure. The synthetic lipids are obtained from peracetyl galactose by a general and versatile procedure based on the trichloroacetimidate methodology. The intense violet fluorescence (376 and 395 nm) and good photostability of pyrene make these compounds highly suitable as probes to study galactolipid metabolism. As proof of concept, we report that compound 2 is a valid tool to detect galactolipase activity in enzymatic preparations of potato tubers. 相似文献
103.
Esra Ilhan‐Ayisigi Pelin Saglam‐Metiner Giuliana Manzi Katharine Giannasi Wim van Hoeve Ozlem Yesil‐Celiktas 《Macromolecular bioscience》2020,20(6)
In this study, the neoplastic drug frequently used in the treatment of lung cancer, carboplatin is loaded to microbubbles via a microfluidic platform. In order to increase the drug loading capacity of microbubbles, carboplatin is encapsulated into alginate polymer layer. The phospholipid microbubbles (MBs) are synthesized by MicroSphere Creator, which is connected with T‐junction and micromixer for the treatment with CaCl2 solution to provide gelation of the alginate coated phospholipid microbubbles (AMBs). The carboplatin loaded alginate coated phospholipid microbubbles (CAMBs) result in 12.2 ± 0.21 µm mean size, obtained by mixing with 0.05% CaCl2 using T‐junction. The cytotoxic activities of the synthesized MBs, AMBs, and CAMBs are also investigated with the 3‐(4,5‐Dimethyl‐2‐thiazolyl)‐2,5‐diphenyl‐2H‐tetrazolium bromide) (MTT) and live/dead fluorescent dying assays in the A549 and BEAS‐2B cell lines. The one‐step microfluidic coating of lipid microbubbles with natural alginate polymer appears to be a promising strategy for enhanced drug reservoir properties. 相似文献
104.
PLA-ZnO nanocomposite films: Water vapor barrier properties and specific end-use characteristics 总被引:1,自引:0,他引:1
Roberto Pantani Giuliana Gorrasi Giovanni Vigliotta Marius Murariu Philippe Dubois 《European Polymer Journal》2013
PLA nanocomposite films with multifunctional characteristics such as mechanical, anti-UV, antibacterial, electrical, gas barrier properties are potentially of high interest as packaging biomaterials. Occasionally, desired and beneficial effects obtained by addition nanofillers come along with some drawbacks, leading to the sharp drop in the molecular weights of the polyester chains, and consequently an important loss of mechanical and thermal properties. Novel PLA-ZnO nanocomposite films were produced by melt-compounding PLA with 0.5–3% ZnO rod-like nanoparticles. The surface treatment of nanofiller by silanization (with triethoxy caprylylsilane) was necessary to obtain a better dispersion and to limit the decrease of molecular mass of PLA. The morphology, molecular, thermo-mechanical and transport properties to water vapor of PLA-ZnO films were analyzed with respect to the neat PLA. According to DSC and to XRD, the produced films were essentially amorphous. The changes in PLA permeation properties were strongly dependent on temperature and nanofiller loading. The well dispersed ZnO nanoparticles within the polyester matrix were effective in increasing the tortuosity of the diffusive path of the penetrant molecules. The activation energy remained similar for PLA and PLA-1% ZnO, but was found greater at higher loading of ZnO (3%), confirming the increased difficulty of travelling molecules to diffuse through PLA. In comparison to the neat PLA (presenting no antimicrobial efficacy), the nanocomposites were active against both Gram-positive and Gram-negative bacteria, stronger antibacterial activity being evidenced after 7 days elapsed time. By considering the multifunctional properties of PLA-ZnO nanocomposites, the films produced by extrusion can be considered a promising alternative as environmental-friendly packaging materials. 相似文献
105.
106.
A method for the comprehensive profiling of the N-acyl-homoserine lactone (AHL) family of bacterial quorum-sensing molecules is presented using liquid chromatography (LC) coupled to a hybrid quadrupole linear ion trap (LTQ) and Fourier-transform ion-cyclotron-resonance mass spectrometer (FTICR). We demonstrate an increase in signal intensity in MS with electrospray ionization (ESI) of the protonated molecules, [M + H](+), by using acetonitrile (ACN) instead of methanol (MeOH) as the organic solvent under the conditions in which the samples were supplied to the probe by direct infusion at constant flow rates. The presence of ACN prevents the formation of methanol adducts such as [M + MeOH + H](+) and [M + MeOH + Na](+), while also lowering the signal intensity of sodiated [M + Na](+) ions. Sensitivity of these signaling molecules in terms of signal-to-noise ratio (S/N) using low-resolution LTQ-MS and high-resolution FTICR-MS were compared under reversed-phase (RP) LC separations with ESI interface. Special emphasis was paid to the choice of the separation column, its elution conditions and detection of the major AHL compounds produced by the Serratia liquefaciens strain ATCC 27592. The most promising results were obtained using a RP C16-amide column eluted with a linear mobile phase gradient ACN/H(2)O containing 0.1% formic acid. The whole set of AHL homologs in bacterial extracts was detected in the extracted-ion chromatographic (XIC) mode, and the calculations of molecular formulae were performed by including the isotopic pattern. This mode of displaying data, with a very narrow mass-to-charge ratio window (i.e. +/- 0.0010 as m/z unit) around each selected ion, has allowed the identification of all the eight known homoserine lactones, viz. C(4)-HSL, 3-oxo-C(6)-HSL, C(6)-HSL, 3-oxo-C(8)-HSL, C(8)-HSL, C(10)-HSL, C(12)-HSL and C(14)-HSL. In addition, at least four uncommon signaling mediators previously unreported, namely, 3-oxo-C(10:1)-HSL, 3-oxo-C(11:2)-HSL, 3-oxo-C(13:2)-HSL and 3-OH-C(16)-HSL, were identified and characterized; their roles in cell-to-cell communication has to be elucidated. 相似文献
107.
Cutignano A Avila C Domenech-Coll A d'Ippolito G Cimino G Fontana A 《Organic letters》2008,10(14):2963-2966
The biosynthesis of lignarenones 1 and 2, the major polyketides of the Mediterranean mollusc Scaphander lignarius is described. The process is primed by benzoic acid and requires acetate and propionate as extender units. The labeling pattern suggests PKS-like synthesis of an unusual E,Z,E-triene chain and origin of the benzoate unit from phenylalanine. 13C-13C NMR COSY has been used to establish the labeling positions due to incorporation of 13C2-acetate. 相似文献
108.
Stefano Gambardella Giuliana Longo Paola Borgiani Federica Sangiuolo Giuseppe Novelli Emiliano Giardina 《Electrophoresis》2016,37(5-6):860-864
The hypoacusia can be classified in two clinical forms: Syndromic (SHL) and Nonsyndromic (NSHL). In particular, the NSHL describes the 70–80% of hypoacusia cases and it is mainly due to genetic factors, which are causative of the deafness at the birth. The genetic hypoacusia presents different inheritance patterns: autosomal dominant (20%), autosomal recessive (80%), X‐linked (1%), and mitochondrial (1%), respectively. To date, about 35 deafness‐causative genes have been identified and most of them codify for connexin transmembrane proteins. Approximately 1:2500 children with NSHL carries mutations in the GJB2 and GJB6 (13q12) genes, which code for connexin 26 (Cx26) and connexin 30 (Cx30), respectively. In the Caucasian population, the most common mutations are 35delG, M34T and 167delT, and D13S1830. Given the frequency distribution of the four mutations in the Caucasian population and the pathogenic connection with NSHL, the development of accurate, rapid, and “low‐cost” molecular assays should be strongly encouraged. To this purpose, we set up two different molecular assays (namely the Cx26 and Cx26‐30 molecular assays) for the fast and inexpensive detection of 35delG, M34T, 167delT, and D13S1830 mutations. Both the molecular approaches showed to be accurate, sensitive, reproducible, and “low‐cost” alternatives for the proper evaluation of the GJB2 and GJB6 genes, which are causative of NSHL. In conclusion, the Cx26 and Cx26‐30 molecular assays can be applied to individual, preconception, prenatal, or postnatal screening for the causative‐mutations of NSHL. 相似文献
109.
Dr. Giuliana Niro Stefanie C. Weck Prof. Dr. Christian Ducho 《Chemistry (Weinheim an der Bergstrasse, Germany)》2020,26(70):16875-16887
To overcome bacterial resistances, the need for novel antimicrobial agents is urgent. The class of so-called nucleoside antibiotics furnishes promising candidates for the development of new antibiotics, as these compounds block a clinically unexploited bacterial target: the integral membrane protein MraY, a key enzyme in cell wall (peptidoglycan) biosynthesis. Nucleoside antibiotics exhibit remarkable structural diversity besides their uridine-derived core motifs. Some sub-classes also show specific selectivities towards different Gram-positive and Gram-negative bacteria, which are poorly understood so far. Herein, the synthesis of a novel hybrid structure is reported, derived from the 5′-defunctionalized uridine core moiety of muraymycins and the peptide chain of sansanmycin B, as a new scaffold for the development of antimicrobial agents. The reported muraymycin–sansanmycin hybrid scaffold showed nanomolar activity against the bacterial target enzyme MraY, but displayed no significant antibacterial activity against S. aureus, E. coli, and P. aeruginosa. 相似文献
110.
Mazzucchelli I Rapetti M Fattore C Franco V Gatti G Perucca E 《Analytical and bioanalytical chemistry》2011,401(3):1013-1021
The development of a simple and rapid high-performance liquid chromatography (HPLC) method for the determination of the new
antiepileptic drug rufinamide (RFN) in human plasma and saliva is reported. Samples (250 μl) are alkalinized with ammonium
hydroxide (pH 9.25) and extracted with dichloromethane using metoclopramide as internal standard. Separation is achieved with
a Spherisorb silica column (250 × 4.6 mm i.d., 5 μm) at 30 °C using as mobile phase a solution of methanol/dichloromethane/n-hexane
10/25/65 (vol/vol/vol) mixed with 6 ml ammonium hydroxide. The instrument used was a Shimadzu LC-10Av chromatograph and flow
rate was 1.5 ml min-1, with a LaChrom L-7400 UV detector set at 230 nm. Calibration curves are linear [r
2 = 0.998 ± 0.002 for plasma (n = 10) and r
2 = 0.999 ± 0.001 for saliva (n = 9)] over the range of 0.25–20.0 μg ml-1, with a limit of quantification at 0.25 μg ml-1. Precision and accuracy are within current acceptability standards. The assay is suitable for pharmacokinetic studies in
humans and for therapeutic drug monitoring. 相似文献