2274-11-5Relevant articles and documents
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.
, p. 4523 - 4526 (2016)
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.
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.
FLEXIBLE TO RIGID NANOPOROUS POLYURETHANE-ACRYLATE (PUAC) TYPE MATERIALS FOR STRUCTURAL AND THERMAL INSULATION APPLICATIONS
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, (2015/11/03)
Novel urethane-acrylate (UAC) Star monomers and polyurethane-acrylate (PUAC) aerogel polymers derived therefrom are described herein, along with other novel, related monomers and polymers. Also described herein are processes for preparing the UAC Star monomers, the PUAC aerogel polymers, and the other related monomers and polymers. The PUAC and related polymers herein are useful in various applications including in structural and thermal insulation.
