The BODIPY family fluorophores have been covalently linked to numerous classes of biomolecules, including proteins, carbohydrates, fatty acids, and steroids. Still, only two research papers on the synthesis and fluorescent biological analysis of BODIPY-labeling of triterpenoid compounds have been reported so far. In these works, fluorescent pentacyclic triterpene conjugates have been prepared by covalent binding to the known BODIPY-FL fluorophore through the 3-OH and 17-COOH functional groups. Here we aimed to work out a new approach for the synthesis of BODIPY-triterpenoid acids conjugates avoiding covalent binding of the triterpene core to the BODIPY-platform at the C-3 and C-17 positions. Novel BODIPY-lupane triterpenoid conjugates bearing a fluorescent marker at the C-2 position of ring A of the triterpene core were obtained via the Sonogashira reaction as a key step. The starting compounds in the cross-coupling reaction were C-2 propynyl derivatives of betulinic or betulonic acids and fluorescent dyes with an iodo-group at C-2 or meso position of BODIPY-platform. The elaborated coupling procedure might have applicability in the synthesis of fluorescent-labeled triterpenoid conjugates suitable for biological assays

Confocal laser scanning microscopy (CSLM) is a powerful microscopic tool that gives valuable morphological and functional information within cells and tissues. CLSM is non-invasive, with high-contrast scanning, a simple and fast sample preparation procedure as well as easy operation. The aim of this paper was to study the intracellular uptake of polymeric nanoparticles loaded with cardiovascular drugs using confocal laser scanning microscopy. Polymeric nanoparticles were prepared via nanoprecipitation method using poly(lactide-co-glycolide) (PLGA) as biodegradable polymeric matrix and Pluronic F127 as a stabilizer. A mixture of two cardiovascular drugs - valsartan (an angiotensin II receptor antagonist drug) and amlodipine besylate (a calcium channel blocker) - was loaded in polymeric nanoparticles. The prepared polymeric nanoparticles had sizes lower than 300 nm and narrow dispersity. The cellular uptake of polymeric nanoparticles was investigated by incubating adherent mouse embryo fibroblasts (NIH 3T3) with a suspension of nanoparticles (stained previously with phthalocyanine) at three different time points. Targeted cell compartments were labeled with two fluorophores: Rhodamine B (membrane stain) and Hoechst (nucleic acid stain). Live cell imaging was performed using a confocal microscope Zeiss LSM710 with Zeiss PALM microdissection system. The intracellular uptake of polymeric nanoparticles was revealed by confocal laser scanning microscopy for each incubation time. The results suggest a possible mechanism of endocytosis and clearly a vesicular-based accumulation of the nanoparticles in the cytoplasmatic compartments .

Easily available 2-(bis(alkylthio)methylene)malononitriles react with cyanoacetamide or cyanothioacetamide to give 4-(alkylthio)-6-amino-2-oxo(thioxo)-1,2-dihydropyridine-3,5-dicarbonitriles. Upon treatment with primary amines and/or HCHO, the compounds undergo heterocyclization to afford new pyrido[1,2-а][1,3,5]triazines or ring-condensed 1,3,5,7-tetrazocine derivatives.

The micellar effect on a Diels-Alder reaction (DA) was analyzed taking advantage of the property presented by Ionic Liquids (ILs) based on 1-alkyl-3-methylimidazolium cations by having amphiphilic character when the alkyl group is a long hydrocarbon chain -12 carbon atoms [C₁₂mim]-. These ILs can act as surfactants forming micelles in aqueous solution.

The reactive system studied consists of nitrofuran and isoprene which allows obtaining benzofuran through green synthetic strategie.

These “new microheterogeneous systems” would allow a better solubilization of non-polar substrates and to adopt reaction conditions softer than the traditional thermal.

A set of 18 imine-phenylaminopyrimidines (imine-PAP) 10a-r against the main protease of SARS-CoV-2, is presented. In addition, these compounds have been previously reported by our group. The best receptor-ligand interactions were obtained from 10i, 10m and 10o as shown by their predicted free Gibbs energy of -9.83, -9.71 and -9.02 kcal/mol respectively. This is in comparison with the co-crystalized ligand in the main protease ( -7.78 kcal/mol,). These results provide solid foundation in order to test the imine-PAP compounds in in vitro studies in order to explore the possible inhibition of the main protease of SARS-CoV-2.