Stimuli responsive lipids, which enable control over the formation, transformation, and disruption of supramolecular assemblies, are of interest for biosensing, diagnostics, drug delivery, and basic transmembrane protein studies. In particular, spatiotemporal control over a supramolecular struct...

Short-chain fatty acids (SCFAs) are one class of bacterial metabolites mainly formed by gut microbiota from undigested fibers and proteins. These molecules are able to mediate signal conduction processes of cells, acting as G protein-coupled receptors (GPR) activators and histone deacetylases (H...

The uranium enrichment of the environmental sample should be analyzed to verify the declared information for the nuclear safeguards. The High-Resolution Gamma Spectrometry (HRGS) and Monochromatic Micro X-ray Fluorescence (MMXRF) is able to analyze the sample with a short detection time and high...

This work highlights the possibility of improving, for given deposited quantities, the accuracy of uranium isotope ratio determination by Thermal Ionization Mass Spectrometry (TIMS) using Faraday cups coupled to a 1012 Ω current amplifying system. This system improves the electronic sensitivity...

The article presents the results of a calculation-to-experiment (C/E) discrepancy analysis for a new evaluation of differential (measuring neutron transmission) and integral experiments from the International Handbook of Evaluated Criticality Benchmark Safety Experiments. The experiments were ca...

The expected growing population and challenges associated with globalisation will increase local food and feed demands and enhance the pressure on local and regional upland soil resources. In light of these potential future developments it is necessary to define sustainable land use and tolerabl...

Reaction of 4-aminobenzonitrile with 2-bromo-4-chlorobutyryl bromide in the presence of sodium phosphate followed by treatment of the coupled product with sodium hydroxide followed by ammonium hydroxide in acetonitrile yielded the title compound as the racemic (R)-(−)-mandelic acid salt in an ov...

Racemic ethyl 3-amino-3-(4-cyanophenyl)propanoate was synthesized and the enantiomers separated through enantioselective N-acylation by Candida antarctica lipase A (CAL-A) in neat butyl butanoate. The free amino acid enantiomers were transformed to the Boc and Fmoc-protected derivatives.

Three copper(II) complexes of aminoquinoline derivatives, l-glycine-N′-8-quinolylamide (L1), l-alanine-N′-8-quinolylamide (L2), and N-(8-quinolyl) pyridine-2-carboxamide (L3) have been shown to cleave plasmid DNA pBR322 and pUC18 with or without the presence of H2O2/ascorbate. Crystallographic...

Six dimeric 2-(2-naphthyl)quinolin-4-amines with a linker between the amino groups and eight dimeric 2-(4-anilino)quinolin-4-amines linked between the anilino groups were synthesized and evaluated for their interaction with duplex/triplex DNA's and as antagonists of immunostimulatory oligod...

Recently, the asymmetric synthesis and biological activity of (R)- and (S)-4-aminoquinolinemethanols 1 as mefloquine analogues were reported. Several compounds showed very promising antimalarial activity, in the nanomolar range, against Plasmodium falciparum 3D7 and W2. Enantiomers with an (S)-a...

Hybrid compounds may play a critical role in the context of the malaria eradication agenda, which will benefit from therapeutic tools active against the symptomatic erythrocytic stage of Plasmodium infection, and also capable of eliminating liver stage parasites. To address the need for efficien...

Malaria remains a major disease in the developing world and globally is the most important parasitic disease causing significant morbidity and mortality. Because of widespread resistance to conventional antimalarials, including chloroquine (CQ), new drugs are urgently needed. Here we report on t...

Eight derivatives of 4-aminoquinolines differing in the substituents attached to the C(4)-amino group and C(7) were synthesised and tested as inhibitors of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Both enzymes were inhibited by all of the compounds with inhibition cons...

Despite years of investigation, pathogenesis of necrotizing enterocolitis (NEC) remains elusive. Bacterial metabolites were implicated by several authors but their roles remain controversial. The aim of our study was to investigate the role of SCFAs and polyamines through a kinetic study of hist...

BackgroundValproic acid (VPA) exposure in utero has been associated with an increased risk of both neural tube defects and autism spectrum disorders (ASDs). The terata induced by VPA suggest interference with pattern formation. Retinoic acid produces similar terata and is known to act in part by...

(−)-(R)-2-methyl-3-(1-pyrrolidinyl)-4′-trifluoromethylpropiophenone monohydrochloride, lanperisone hydrochloride (NK433) administered intravenously or orally depressed the mono- and polysynaptic reflex potential, dorsal root reflex potential, flexor reflex mediated by group II afferent fibers, ...

A Et3N-mediated Neber reaction of aryl/alkyl-2,2,2-trifluoroethylketoximes has been developed. This one-pot metal-free protocol enables the facile construction of an array of trifluoromethyl-substituted azirines in moderate to high yields under mild reaction conditions. Further transformations o...

Several peptide fragments representing N-terminal, C-terminal, and internal sequences of [Leu13]porcine motilin ([Leu13]pMOT) were synthesized using Fmoc solid phase methodology. Peptides were assayed for motilin receptor binding activity in a rabbit antrum smooth muscle preparation and for stim...

We describe the antagonistic properties due to the replacement of Pro3 by phenylalanine in porcine motilin. The analogue, [Phe3,Leu13]porcine motilin (OHM-11526), displaces iodinated [Nle13]porcine motilin bound to a homogenate of rabbit antral smooth muscle tissue. The dissociation constant (pK...