Potent E‐Selectin Antagonists

In the search for drugs that could control excessive leukocyte extravasation, we now report on modifications of the already known potent E‐selectin antagonist 3 containing a cyclohexyllactic acid residue and a glucal‐derived building block. Thus, we describe the synthesis and biological evaluation of a series of derivatives 6 with modified glucal‐derived moieties (CH₂NR¹R² instead of CH₂OH in 3 ) to explore a hypothetical potential complementary interaction with E‐selectin. However, similar activity profiles of most derivatives 6 and compound 3 do not support such an interaction, but rather indicate topological‐structure changes of 6 (and 3 ) in the orientation of the neighboring fucose and galactose due to intramolecular steric interactions. The most potent E‐selectin antagonist 6v showed >50‐fold improved E‐selectin inhibition compared to the weak selectin ligand sialyl Lewis^x (sLe^x, 1 ; IC₅₀=1000 – 1500 μM ), but only a 2‐fold improvement compared to 3 . Compound 6x was tested in vivo in a murine model of acute inflammation and found to be as potent as 3 (ED₅₀=15 mg/kg).     

Eine Technik zum Nachweis von Peptiden mit Chlor und o-Tolidin auf Papier

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Papier

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Electro‐Optic (E‐O) Molecular Glasses

This Focus Review describes molecular glasses as a new class of materials for nonlinear optical (NLO) applications, especially for electro‐optic (E‐O) devices. Examples of E‐O molecular glasses are reviewed with a focus on the molecular design of NLO chromophores and solid‐state engineering of molecular glasses. Molecular glasses based on dendrimers of multiple chromophores, molecular glass blends of chromophores, and molecular glasses based on reversible self‐assembly of chromophores are introduced as promising architectures to prepare morphologically stable molecular glasses with large E‐O activities and improved material properties for device applications. Future directions to fully exploit the potential of molecular glasses for NLO materials are presented.     

Papier

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Papier

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