21 research outputs found

    Synthesis and evaluation of ÎČ-hydroxytriazoles and related compounds as antitubercular agents

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    A new series of ÎČ-hydroxytriazoles were synthesized and evaluated as Mycobacterium tuberculosis inhibitors. Our strategy implied the synthesis of alkyne precursors through a Barbier reaction between benzaldehydes and propargyl bromide followed by click chemistry to afford substituted ÎČ-hydroxyl benzyltriazoles. These compounds are also key intermediates either for oxidation reactions leading to α,ÎČ-diketotriazoles or for elimination reactions affording styryl triazoles. Evaluation of all new compounds for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv resulted in compounds with MIC up to 7 ÎŒM

    2-Phenylbenzoxazole derivatives: a family of robust emitters of solid-state fluorescence

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    Mechanofluorochromic Properties of an AIEE-Active 2-Phenylbenzoxazole Derivative: More than Meets the Eye?

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    International audienceThe presence of a dicyanovinyl group on the robust 2‐phenylbenzoxazole framework led to the emergence of aggregation‐induced emission enhancement (AIEE) characteristics. A mechanofluorochromic (MFC) behaviour was observed. The pristine microcrystals emitted yellow‐green light, which became golden yellow upon grinding, with the reverse process observed upon heating or solvent fuming. This phenomenon was accompanied by a reversible evolution of the photoluminescence quantum yields and lifetimes. These variations were attributed to the formation of different types of emissive species in the crystalline phases and in the ground material, which is a mixture of very small microcrystals and amorphous matter. Remarkably, evidence was also given for other spectroscopic effects, which depend on the size, compactness and heterogeneity of the solid samples. These effects are presumably linked to the generation of regions rich in low‐energy exciton traps in polycrystalline and pressed samples, and to light reabsorption. They are enhanced by the fact that the pristine platelets exhibit self‐waveguided edge emission, and they are all the more significant as the MFC effect is rather weak

    The role of the synthetic chromophore of GFP in generating polymorphism-dependent on/off photoluminescence

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    International audiencePolymorphism, i.e. the ability of a solid material to exist in more than one crystal form, gives unique opportunity to study the correlation between the solid-state molecular arrangement and the photoluminescence properties, and allows optimizing the performances of materials with reduced synthesis effort. Compound 1, which results from the combination of 2phenylbenzoxazole (PBO) and benzylideneimidazolinone (BDI), was known to be weakl
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