This study is concerned with the incorporation of surface modified fumed silica nanoparticles (FSNPs) into polymethacrylate based monolithic columns for use in reversed phase chromatography (RPC) of small solutes and proteins. First, FSNPs were modified with 3-(trimethoxysilyl)propylmethacrylate...

This research article presents the preparation and characterization of monolithic capillary columns with incorporated bare fumed silica nanoparticles (FSNPs) and surface coated gluconamide FSNPs and their subsequent use in hydrophilic interaction capillary electrochromatography (HI-CEC) of small...

The aim of this study was to investigate the impact of the addition of magnesium aluminum silicate (MAS), a natural clay, on the properties of polymeric films based on quaternary polymethacrylates (QPMs). Two commercially available aqueous QPM dispersions were studied: Eudragit® RS 30D and Eudra...

The still unknown contribution of the D4 receptors to memory consolidation was studied examining the memory effects of the dopamine D4 agonist PD168,077, the putative dopamine D4 antagonist L745,870, their mutual combination, and the combination of the D4 agonist with representative compounds ac...

A series of phenylpiperazine-methyl-substituted 1H-pyrrolo[2,3-c]pyridine, imidazo[1,2-c]-, pyrrolo[2,3-d]- and pyrrolo[3,2-d]pyrimidines were prepared as selective dopamine D4-ligands. The pyrrolo[2,3-d]pyrimidine derivatives 12d (Ki = 1,9 nM) and 34d (Ki = 2,4 nM) as well as the pyrrolo[3,2-d]...

A new critical point symmetry (CPS) for odd-even systems is developed through coupling the T(4) CPS to a single particle within a spherical-j orbit. The resulting model is shown to be exactly solvable and serve as the triaxial CPS for transitional odd-A nuclei. A comparison between the model cal...

Ternary organic solar cells (OSCs) are very promising because they can further enhance the photons’ utilization efficiencies of binary cells. Herein, we design and synthesize three linear A-π-A-π-A (A: electron acceptor) small molecules (SMs) BTTR, BT2TR and BT3TR with a 2,1,3-benzothiadiazol...

Although the relative performance of sensory discrimination methods is well theorized in Thurstonian modeling and signal detection theory (SDT), empirical research is needed to investigate how such theorized models could be validated in complex sensory testing situations of food and beverages. T...

BackgroundHuman infection by Acinetobacter baumannii has been increased due to its resistance against most of the antibiotics. Therefore, the present study aimed to design a candidate vaccine against A. baumannii infection.

Alkylation of aromatic rings is a major challenge in organic syntheses since more complex carbon skeletons can be constructed. The alkylation of pyridine by nucleophilic aromatic substitution of the nitro group in methyl 3-nitro-4-pyridylcarboxylate (1) with malonic ester is reported. The versat...

The reaction of vinyl selenones with di-(−)-bornyl malonate and sodium hydride occurred with low diastereoselectivity and afforded a mixture of two diastereomeric cyclopropane derivatives in comparable yields. These, however, could be easily separated by chromatography. Removal of the bornyl gro...

Hemisynthesis of methyl pyrethroates from γ-alkoxy-alkylidene malonates and isopropylidenediphenylsulfurane and isopropylidenetriphenylphosphorane is disclosed. It takes advantage of the high degree of stereocontrol observed in the cyclopropanation of γ-alkoxy-alkylidene malonates by the above...

A novel and practical synthesis of dinotefuran 1, featuring a new access to it from known key intermediate (tetrahydrofuran-3-yl)-methanamine 5, has been achieved through Michael addition reaction of nitromethane to diethyl maleate in 6 steps with 45.5% total yield. This synthesis is scalable an...

Monofluoroalkenes bearing a malonate unit at the β position can be synthesized by the enantioselective addition of diesters to 3,3-difluoropropenes. The difference in reactivity regarding the geometry and the substituents of the alkene of the 3,3-difluoropropenes, as well as the alkyl groups of...

We disclose a new microwave-assisted protocol for the effective α-arylation of diethyl malonate. The coupling of aryl halides with diethyl malonate proceeds smoothly in short reaction time in the presence of a catalytic amount of Cu(OTf)2, 2-picolinic acid and Cs2CO3 in toluene using microwave ...

The heptapropionates 5 and 20 were synthesised by iterative application of the boronmediated aldol reaction of ethyl ketone (R)-4 and subsequent reduction. Polyketide library diversification was realised by varying the ketone configuration and substitution in the aldol bond constructions.

A new enzyme catalysed kinetic resolution of cis-4-benzyloxy-2,3-epoxybutanol has been reported. Efficient, scalable separation of the optically active alcohol from its ester derivative has been solved with liquid–liquid and solid–liquid extraction methods using commercial organic solvents and...

The exclusive distribution of 5-HT6 receptor in the brain regions and high affinity for antipsychotic and antidepressant drugs makes 5-HT6 receptor a promising target in treatment of CNS diseases. Based on a pharmacophore model reported in the literature, we designed and synthesized a novel seri...

Twenty-four compounds of 4-methoxy-N-[3-(4-substituted phenyl-piperazine-1-yl)propyl] benzene sulfonamides and N-[3-(4-substituted phenyl-piperazine-1-yl)propyl] naphthyl sulfonamides were prepared and evaluated as 5-HT7 receptor antagonists. Most of the compounds showed the IC50 values of 12–5...

A structure-based virtual screening of commercial compounds was carried out on the HCV NS3 helicase structure, with the aim to identify novel inhibitors of HCV replication. Among a selection of 13 commercial structures, one compound was found to inhibit the subgenomic HCV replicon in the low mic...