26570-48-9Relevant articles and documents
A facile approach to bis(Isoxazoles), promising ligands of the ampa receptor
Averina, Elena B.,Grigoriev, Vladimir V.,Grishin, Yuri K.,Karlov, Dmitry S.,Kuznetsova, Tamara S.,Palyulin, Vladimir A.,Radchenko, Eugene V.,Rybakov, Victor B.,Sadovnikov, Kirill S.,Sedenkova, Kseniya N.,Vasilenko, Dmitry A.,Zamoyski, Vladimir L.
, (2021/11/01)
A convenient synthetic approach to novel functionalized bis(isoxazoles), the promising bivalent ligands of the AMPA receptor, was elaborated. It was based on the heterocyclization reactions of readily available electrophilic alkenes with the tetranitromethane-triethylamine complex. The structural diversity of the synthesized compounds was demonstrated. In the electrophysi-ological experiments using the patch clamp technique on Purkinje neurons, the compound 1,4-phenylenedi(methylene)bis(5-aminoisoxazole-3-carboxylate) was shown to be highly potent positive modulator of the AMPA receptor, potentiating kainate-induced currents up to 70% at 10?11 M.
Synthesis and activity of novel homodimers of Morita–Baylis–Hillman adducts against Leishmania donovani: A twin drug approach
da Silva, Wagner A.V.,Rodrigues, Daniele C.,de Oliveira, Ramon G.,Mendes, Rhuan K.S.,Olegário, Tayná R.,Rocha, Juliana C.,Keesen, Tatjana S.L.,Lima-Junior, Claudio G.,Vasconcellos, Mário L.A.A.
supporting information, p. 4523 - 4526 (2016/08/24)
It is reported here the synthesis of novel Homodimers 12–19 of Morita–Baylis–Hillman adducts (MBHA) from one-pot Morita–Baylis–Hillman Reaction (MBHR) between aromatic aldehydes as eletrophiles and ethylene glycol diacrylate as Michael acceptor (35–94% yields) using cheap and green conditions. The bioactivities were evaluated against promastigote form of Leishmania donovani. All homodimers showed to be more potent than corresponding monomers. It is worth highlighting that the halogenated homodimers 17 and 18 (0.50?μM) is almost 400 times more active than the corresponding monomer 10 and 1.24 times more potent than the second-line drug amphotericin B (0.62?μM). Moreover, the selectivity index to 18 is very high (SIrb?>?400) far better than amphotericin B (SIrb?=?18.73). This is the first report of twin drugs strategy applied on Morita–Baylis–Hillman adducts.
Method for synthesizing (methyl) acrylate glyceride through catalysis of calcium glyceroxide
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Paragraph 0041; 0042, (2017/09/14)
The invention discloses a method for synthesizing (methyl) acrylate glyceride through catalysis of calcium glyceroxide and belongs to the field of fine chemical engineering. The method comprises the steps that a reaction-rectification technology is adopted, a refit rectification column filled with copper wire gauze is used, and alkyl (meth) acrylate, glycerol, a polymerization inhibitor and a catalyst are added; under the string condition, air is introduced, and heating is carried out until a reaction solution flows back, wherein the temperature ranges from 60 DEG C to 140 DEG C; after the reaction is finished, a reaction solution is cooled to 50 DEG C, active carbon is added, stirring is continuously carried out for 0.5-1 h with the temperature maintained, the reaction solution is subjected to pressure reduction suction filtration after the reaction is finished, filter liquor is subjected to pressure reduction rotary steaming to remove the excessive raw material ester, and the (methyl) acrylate glyceride reactive diluent product is obtained. The method overcomes the defects of an existing ester exchange catalyst, and is high in yield, simple in aftertreatment and easy to implement.
