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Sökning: L773:2191 1363

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1.
  • Andersson, Per Ola, et al. (författare)
  • Towards Fingermark Dating : A Raman Spectroscopy Proof-of-Concept Study
  • 2017
  • Ingår i: ChemistryOpen. - : Wiley. - 2191-1363. ; 6:6, s. 706-709
  • Tidskriftsartikel (refereegranskat)abstract
    • Fingermarks have, for a long time, been vital in the forensic community for the identification of individuals, and a possibility to non-destructively date the fingermarks would of course be beneficial. Raman spectroscopy is, herein, evaluated for the purpose of estimating the age of fingermarks deposits. Well-resolved spectra were non-destructively acquired to reveal spectral uniqueness, resembling those of epidermis, and several molecular markers were identified that showed different decay kinetics: carotenoids > squalene > unsaturated fatty acids > proteins. The degradation rates were accelerated, less pronounced for proteins, when samples were stored under ambient light conditions, likely owing to photo-oxidation. It is hypothesized that fibrous proteins are present and that oxidation of amino acid side chains can be observed both through Raman and fluorescence spectroscopy. Clearly, Raman spectroscopy is a useful technique to non-destructively study the aging processes of fingermarks.
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2.
  • Arja, Katriann, et al. (författare)
  • Synthesis and Characterization of Novel Fluoro-glycosylated Porphyrins that can be Utilized as Theranostic Agents
  • 2018
  • Ingår i: ChemistryOpen. - : Wiley-VCH Verlagsgesellschaft. - 2191-1363. ; 7:7, s. 495-503
  • Tidskriftsartikel (refereegranskat)abstract
    • Small molecules with modalities for a variety of imaging techniques as well as therapeutic activity are essential, as such molecules render opportunities to simultaneously conduct diagnosis and targeted therapy, so called theranostics. In this regard, glycoporphyrins have proven useful as theranostic agents towards cancer, as well as noncancerous conditions. Herein, the synthesis and characterization of heterobifunctional glycoconjugated porphyrins with two different sugar moieties, a common monosaccharide at three sites, and a 2-fluoro-2-deoxy glucose (FDG) moiety at the fourth site are presented. The fluoro-glycoconjugated porphyrins exhibit properties for multimodal imaging and photodynamic therapy, as well as specificity towards cancer cells. We foresee that our findings might aid in the chemical design of heterobifunctional glycoconjugated porphyrins that could be utilized as theranostic agents.
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3.
  • Behrends, Malte, et al. (författare)
  • N-Aryl Isoleucine Derivatives as Angiotensin II AT(2) Receptor Ligands
  • 2014
  • Ingår i: ChemistryOpen. - : Wiley. - 2191-1363. ; 3:2, s. 65-75
  • Tidskriftsartikel (refereegranskat)abstract
    • A novel series of ligands for the recombinant human AT(2) receptor has been synthesized utilizing a fast and efficient palladium-catalyzed procedure for aminocarbonylation as the key reaction. Molybdenum hexacarbonyl [Mo(CO)(6)] was employed as the carbon monoxide source, and controlled microwave heating was applied. The prepared N-aryl isoleucine derivatives, encompassing a variety of amide groups attached to the aromatic system, exhibit binding affinities at best with K-i values in the low micromolar range versus the recombinant human AT(2) receptor. Some of the new nonpeptidic isoleucine derivatives may serve as starting points for further structural optimization. The presented data emphasize the importance of using human receptors in drug discovery programs.
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4.
  • Bielawski, Marcin, et al. (författare)
  • One-Pot Synthesis and Applications of N-Heteroaryl Iodonium Salts
  • 2014
  • Ingår i: ChemistryOpen. - : Wiley. - 2191-1363. ; 3:1, s. 19-22
  • Tidskriftsartikel (refereegranskat)abstract
    • An efficient one-pot synthesis of N-heteroaryl iodonium triflates from the corresponding N-heteroaryl iodide and arene has been developed. The reaction conditions resemble our previous one-pot syntheses, with suitable modifications to allow N-heteroaryl groups. The reaction time is only 30min, and no anion exchange is required. The obtained iodonium salts were isolated in a protonated form, these salts can either be employed directly in applications or be deprotonated prior to use. The aryl groups were chosen to induce chemoselective transfer of the heteroaryl moiety to various nucleophiles. The reactivity and chemoselectivity of these iodonium salts were demonstrated by selectively introducing a pyridyl moiety onto both oxygen and carbon nucleophiles in good yields.
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5.
  • Borhade, Sanjay R, et al. (författare)
  • Inhibition of Insulin-Regulated Aminopeptidase (IRAP) by Arylsulfonamides
  • 2014
  • Ingår i: ChemistryOpen. - : Wiley. - 2191-1363. ; 3:6, s. 256-263
  • Tidskriftsartikel (refereegranskat)abstract
    • The inhibition of insulin-regulated aminopeptidase (IRAP, EC 3.4.11.3) by angiotenesin IV is known to improve memory and learning in rats. Screening 10 500 low-molecular-weight compounds in an enzyme inhibition assay with IRAP from Chinese Hamster Ovary (CHO) cells provided an arylsulfonamide (N-(3-(1H-tetrazol-5-yl)phenyl)-4-bromo-5-chlorothiophene-2-sulfonamide), comprising a tetrazole in the meta position of the aromatic ring, as a hit. Analogues of this hit were synthesized, and their inhibitory capacities were determined. A small structure-activity relationship study revealed that the sulfonamide function and the tetrazole ring are crucial for IRAP inhibition. The inhibitors exhibited a moderate inhibitory potency with an IC50=1.1±0.5 μm for the best inhibitor in the series. Further optimization of this new class of IRAP inhibitors is required to make them attractive as research tools and as potential cognitive enhancers.
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6.
  • Bäck, Marcus, et al. (författare)
  • Tyrosine Side-Chain Functionalities at Distinct Positions Determine the Chirooptical Properties and Supramolecular Structures of Pentameric Oligothiophenes
  • 2020
  • Ingår i: ChemistryOpen. - : Wiley. - 2191-1363. ; 9:11, s. 1100-1108
  • Tidskriftsartikel (refereegranskat)abstract
    • Control over the photophysical properties and molecular organization of pi-conjugated oligothiophenes is essential to their use in organic electronics. Herein we synthesized and characterized a variety of anionic pentameric oligothiophenes with different substitution patterns of L- or D-tyrosine at distinct positions along the thiophene backbone. Spectroscopic, microscopic, and theoretical studies of L- or D-tyrosine substituted pentameric oligothiophene conjugates revealed the formation of optically active pi-stacked self-assembled aggregates under acid conditions. The distinct photophysical characteristics, as well as the supramolecular structures of the assemblies, were highly influenced by the positioning of the L- or D-tyrosine moieties along the thiophene backbone. Overall, the obtained results clearly demonstrate how fundamental changes in the position of the enantiomeric side-chain functionalities greatly affect the optical properties as well as the architecture of the self-assembled supramolecular structures.
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7.
  • Chen, Shujing, et al. (författare)
  • Manufacturing Graphene-Encapsulated Copper Particles by Chemical Vapor Deposition in a Cold Wall Reactor
  • 2019
  • Ingår i: ChemistryOpen. - : Wiley. - 2191-1363. ; 8:1, s. 58-63
  • Tidskriftsartikel (refereegranskat)abstract
    • Functional fillers, such as Ag, are commonly employed for effectively improving the thermal or electrical conductivity in polymer composites. However, a disadvantage of such a strategy is that the cost and performance cannot be balanced simultaneously. Therefore, the drive to find a material with both a cost efficient fabrication process and excellent performance attracts intense research interest. In this work, inspired by the core-shell structure, we developed a facile manufacturing method to prepare graphene-encapsulated Cu nanoparticles (GCPs) through utilizing an improved chemical vapor deposition (CVD) system with a cold wall reactor. The obtained GCPs could retain their spherical shape and exhibited an outstanding thermal stability up to 179 degrees C. Owing to the superior thermal conductivity of graphene and excellent oxidation resistance of GCPs, the produced GCPs are practically used in a thermally conductive adhesive (TCA), which commonly consists of Ag as the functional filler. Measurement shows a substantial 74.6 % improvement by partial replacement of Ag with GCPs.
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8.
  • Chien, Yu-Chuan, 1990-, et al. (författare)
  • Poly(Ethylene Glycol-block-2-Ethyl-2-Oxazoline) as Cathode Binder in Lithium-Sulfur Batteries
  • 2021
  • Ingår i: ChemistryOpen. - : John Wiley & Sons. - 2191-1363. ; 10:10, s. 960-965
  • Tidskriftsartikel (refereegranskat)abstract
    • Functional binders constitute a strategy to overcome several challenges that lithium-sulfur (Li-S) batteries are facing due to soluble reaction intermediates in the positive electrode. Poly (ethylene oxide) (PEO) and poly (vinylpyrrolidone) (PVP) are in this context a previously well-explored binder mixture. Their ether and amide groups possess affinity to the dissolved sulfur species, which enhances the sulfur utilization and mitigates the parasitic redox shuttle. However, the immiscibility of PEO and PVP is a concern for electrode stability. Copolymers comprising ether and amide groups are thus promising candidates to improve the stability the system. Here, a series of poly (ethylene glycol-block-2-ethyl-2-oxazoline) with various block lengths is synthesized and explored as binders in S/C composite electrodes in Li-S cells. While the electrochemical analyses show that although the sulfur utilization and capacity retention of the tested electrodes are similar, the integrity of the as-cast electrodes can play a key role for power capability.
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9.
  • Deiana, Luca, 1982-, et al. (författare)
  • Direct Catalytic Asymmetric Synthesis of Pyrazolidine Derivatives
  • 2012
  • Ingår i: ChemistryOpen. - : Wiley. - 2191-1363. ; 1:3, s. 134-139
  • Tidskriftsartikel (refereegranskat)abstract
    • A highly enantioselective, metal-free cascade reaction between di-1,2-N-protected hydrazine and α,β-unsaturated aldehydes is disclosed. The catalytic, asymmetric cascade transformation is a direct entry to 3-hydroxypyrazolidine and 3-allylpyrazolidine derivatives in one step and two steps, respectively, with >19:1 d.r. and 98–99 % ee using simple chiral pyrrolidines as catalysts.
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10.
  • Engen, Karin, et al. (författare)
  • Synthesis, Evaluation and Proposed Binding Pose of Substituted Spiro-Oxindole Dihydroquinazolinones as IRAP Inhibitors
  • 2020
  • Ingår i: ChemistryOpen. - : Wiley. - 2191-1363. ; 9:3, s. 325-337
  • Tidskriftsartikel (refereegranskat)abstract
    • Insulin‐regulated aminopeptidase (IRAP) is a new potential macromolecular target for drugs aimed for treatment of cognitive disorders. Inhibition of IRAP by angiotensin IV (Ang IV) improves the memory and learning in rats. The majority of the known IRAP inhibitors are peptidic in character and suffer from poor pharmacokinetic properties. Herein, we present a series of small non‐peptide IRAP inhibitors derived from a spiro‐oxindole dihydroquinazolinone screening hit (pIC50 5.8). The compounds were synthesized either by a simple microwave (MW)‐promoted three‐component reaction, or by a two‐step one‐pot procedure. For decoration of the oxindole ring system, rapid MW‐assisted Suzuki‐Miyaura cross‐couplings (1 min) were performed. A small improvement of potency (pIC50 6.6 for the most potent compound) and an increased solubility could be achieved. As deduced from computational modelling and MD simulations it is proposed that the S‐configuration of the spiro‐oxindole dihydroquinazolinones accounts for the inhibition of IRAP.
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