Amphetamine-like Deferiprone and Clioquinol Derivatives as Iron Chelating Agents.

The accumulation of iron in dopaminergic neurons can cause oxidative stress and dopaminergic neuron degeneration. Iron chelation therapy may reduce dopaminergic neurodegeneration, but chelators should be targeted towards dopaminergic cells. In this work, two series of compounds based on 8-hydroxyquinoline and deferiprone, iron chelators that have amphetamine-like structures, have been designed, synthesized and characterized.

A metabolic inhibitor blocks cellular fucosylation and enables production of afucosylated antibodies.

The fucosylation of glycoproteins regulates diverse physiological processes. Inhibitors that can control cellular levels of protein fucosylation have consequently emerged as being of high interest. One area where inhibitors of fucosylation have gained significant attention is in the production of afucosylated antibodies, which exhibit superior antibody-dependent cell cytotoxicity as compared to their fucosylated counterparts.

Recent Advances in High-Rate Solar-Driven Interfacial Evaporation.

Recent advances in solar-driven interfacial evaporation (SDIE) have led to high evaporation rates that open promising avenues for practical utilization in freshwater production and industrial application for pollutant and nutrient concentration, and resource recovery. Breakthroughs in overcoming the theoretical limitation of 2D interfacial evaporation have allowed for developing systems with high evaporation rates. This study presents a comprehensive review of various evaporator designs that have achieved pure evaporation rates beyond 4 kg m h, including structural and material designs allowing for rapid evaporation, passive 3D designs, and systems coupled with alternative energy sources of wind and joule heating.

4-Chloroisocoumarins as Chlamydial Protease Inhibitors and Anti-Chlamydial Agents.

4-Chloroisocoumarin compounds have broad inhibitory properties against serine proteases. Here, we show that selected 3-alkoxy-4-chloroisocoumarins preferentially inhibit the activity of the conserved serine protease High-temperature requirement A of . The synthesis of a new series of isocoumarin-based scaffolds has been developed, and their anti-chlamydial properties were investigated.

sp -Rich Heterocycle Synthesis on DNA: Application to DNA-Encoded Library Production.

DNA encoded library (DEL) synthesis represents a convenient means to produce, annotate and store large collections of compounds in a small volume. While DELs are well suited for drug discovery campaigns, the chemistry used in their production must be compatible with the DNA tag, which can limit compound class accessibility. As a result, most DELs are heavily populated with peptidomimetic and sp -rich molecules.

Organic impurity profiling of 3,4-methylenedioxyamphetamine (MDA) synthesised from helional.

The organic impurity profile of 3,4-methylenedioxyamphetamine (MDA) synthesised from helional via the "twodogs" method was examined to identify route-specific and condition-specific impurities. The synthesis used a condensation reaction, followed by a Beckmann rearrangement, then Hofmann rearrangement, and then conversion to a hydrochloride salt. Two chlorinating agents were investigated for the Hofmann rearrangement reaction, trichloroisocyanuric acid (TCCA) and sodium hypochlorite.

Optimized production, purification, and radiolabeling of the Pb/Pb theranostic pair for nuclear medicine.

TRIUMF is one of the only laboratories in the world able to produce both lead-203 (Pb, t = 51.9 h) and Pb (t = 10.6 h) onsite via its 13 and 500 MeV cyclotrons, respectively.

Selective Chelation of the Exotic Meitner-Auger Emitter Mercury-197 m/g with Sulfur-Rich Macrocyclic Ligands: Towards the Future of Theranostic Radiopharmaceuticals.

Mercury-197 m/g are a promising pair of radioactive isomers for incorporation into a theranostic as they can be used as a diagnostic agent using SPECT imaging and a therapeutic via Meitner-Auger electron emissions. However, the current absence of ligands able to stably coordinate Hg to a tumour-targeting vector precludes their use in vivo. To address this, we report herein a series of sulfur-rich chelators capable of incorporating Hg into a radiopharmaceutical.

Comparative Study of a Decadentate Acyclic Chelate, HOPO-O, and Its Octadentate Analogue, HOPO-O, for Radiopharmaceutical Applications.

Radiolanthanides and actinides are aptly suited for the diagnosis and treatment of cancer via nuclear medicine because they possess unique chemical and physical properties (e.g., radioactive decay emissions).

Evaluation of the Effect of Macrocyclic Ring Size on [Pb]Pb(II) Complex Stability in Pyridyl-Containing Chelators.

As an element-equivalent theranostic pair, lead-203 (Pb, 100% EC, half-life = 51.92 h) and lead-212 (Pb, 100% β, half-life = 10.64 h), through the emission of γ rays and an α particle in its decay chain, respectively, can aid in the development of personalized targeted radionuclide treatment for advanced and currently untreatable cancers.

Development of a multi faceted platform containing a tetrazine, fluorophore and chelator: synthesis, characterization, radiolabeling, and immuno-SPECT imaging.

Background: Combining optical (fluorescence) imaging with nuclear imaging has the potential to offer a powerful tool in personal health care, where nuclear imaging offers in vivo functional whole-body visualization, and the fluorescence modality may be used for image-guided tumor resection. Varying chemical strategies have been exploited to fuse both modalities into one molecular entity. When radiometals are employed in nuclear imaging, a chelator is typically inserted into the molecule to facilitate radiolabeling; the availability of the chelator further expands the potential use of these platforms for targeted radionuclide therapy if a therapeutic radiometal is employed.

Dietary vitamin B12 regulates chemosensory receptor gene expression via the MEF2 transcription factor in Caenorhabditis elegans.

Dynamic changes in chemoreceptor gene expression levels in sensory neurons are one strategy that an animal can use to modify their responses to dietary changes. However, the mechanisms underlying diet-dependent modulation of chemosensory gene expression are unclear. Here, we show that the expression of the srh-234 chemoreceptor gene localized in a single ADL sensory neuron type of Caenorhabditis elegans is downregulated when animals are fed a Comamonas aquatica bacterial diet, but not on an Escherichia coli diet.

Highly stable gold nanolayer membrane for efficient solar water evaporation under a harsh environment.

Interfacial solar water evaporation has attracted tremendous attention for sunlight harvesting for water purification. However, salt formation and stability of the photothermal materials (PTMs) remain a challenge that need addressing before bringing this technology to real-world applications. In this work, a nanoscale thin film of gold (Au) on a polytetrafluoroethylene (PTFE) membrane has been prepared using a magnetic sputtering technique.

A long-life lithium-oxygen battery via a molecular quenching/mediating mechanism.

The advancement of lithium-oxygen (Li-O) batteries has been hindered by challenges including low discharge capacity, poor energy efficiency, severe parasitic reactions, etc. We report an Li-O battery operated via a new quenching/mediating mechanism that relies on the direct chemical reactions between a versatile molecule and superoxide radical/LiO. The battery exhibits a 46-fold increase in discharge capacity, a low charge overpotential of 0.

Draft Genome Sequence of a Diploid and Hybrid Strain, UCD423, Isolated from Compost in Ireland.

Candida sanyaensis is a CUG-Ser1 clade yeast that is associated with soil. Assembly of short-read and long-read data shows that C. sanyaensis has a diploid and hybrid genome, with approximately 97% identity between the haplotypes.

Synthesis and Evaluation of Bifunctional [2.2.2]-Cryptands for Nuclear Medicine Applications.

For the first time, synthesis of bifunctional [2.2.2]-cryptands (CRYPT) and demonstration of radiolabeling with lead(II) (Pb) isotopes are disclosed herein.

Raising the Bar: Using Simulation to Advance Staff Competency Regarding the Patient Experience.

This article describes one hospital's use of simulation to improve the knowledge, skills, and abilities of an emergency department team regarding the patient experience. Step-by-step instructions are provided on how to conduct the simulations in a way that allows for the practice of new skills in a safe environment-one that promotes reflection, feedback, and learning.

The impact of the degree of intimate mixing on the compaction properties of materials produced by crystallo-co-spray drying.

Direct compression remains one of the most favourable methods available to produce tablet compacts due to its simplicity, efficiency and cost effectiveness however, the technique still remains unsuitable for the majority of formulations due to materials exhibiting poor physical properties such as inadequate compressibility and deformation mechanisms. Whereas crystallo-co-spray drying of various blends has shown to improve the tabletting properties of poorly processable materials, the role of the solvent feed composition in altering the soluble fraction ratio of the excipient to the drug in a crystallo-co-spray dried agglomerate is not well understood. The aim of this work was to investigate the role of the soluble fraction of a drug (paracetamol) and an excipient (α-lactose monohydrate) on the tabletting properties of their crystallo-co-spray dried agglomerates produced via co-spray drying using various inlet feed solvent compositions in order to vary the soluble fraction of the excipient in the feed.

The Effect of Compositional Changes Due to Seasonal Variation on Milk Density and the Determination of Season-Based Density Conversion Factors for Use in the Dairy Industry.

The objective of this study was to determine the effect of seasonal variation on milk composition and establish an algorithm to predict density based on milk composition to enable the calculation of season-based density conversion calculations. A total of 1035 raw whole milk samples were collected from morning and evening milking of 60 spring-calving individual cows of different genetic groups, namely Jersey, Elite HF (Holstein-Friesian) and National Average HF, once every two weeks for a period of 9 months (March-November, 2018). The average mean and standard deviation for milk compositional traits were 4.

Mechanochemical activation with cyclodextrins followed by compaction as an effective approach to improving dissolution of rutin.

Rutin is one of the most important flavonoids with poor bioavailability. This work aimed at addressing the issue of poor biopharmaceutical performance of rutin by applying a combination of complexation with secondary processing into tablets. Mechanical activation was the most suitable method of rutin complex formation with (2-hydroxypropyl)-β-cyclodextrin (HP-β-CD), while the β-cyclodextrin (β-CD) complex successfully formed by kneading with an ethanol/water mixture.

Validation of an ear tag-based accelerometer system for detecting grazing behavior of dairy cows.

The objective of the study was to develop a grazing algorithm for an ear tag-based accelerometer system (Smartbow GmbH, Weibern, Austria) and to validate the grazing algorithm with data from a noseband sensor. The ear tag has an acceleration sensor, a radio chip, and temperature sensor for calibration and it can monitor rumination and detect estrus and localization. To validate the ear tag, a noseband sensor (RumiWatch, Itin and Hoch GmbH, Liestal, Switzerland) was used.

Organic impurity profiling of 3,4-methylenedioxymethamphetamine (MDMA) synthesised from catechol and eugenol via 4-allylcatechol.

This work examines organic impurity profiles of 3,4-methylenedioxymethamphetamine (MDMA) that has been synthesised from the "pre-precursors" catechol (1,2-dihydroxybenzene) and eugenol, via a safrole intermediate. MDMA was synthesised from the catechol- and eugenol-derived safrole intermediate via two routes, which resulted in the synthesis of MDMA from catechol via two routes (Route 1A and 1B) and from eugenol via two routes (Route 2A and 2B). Twelve organic impurities were identified in MDMA synthesised via Routes 1A and 1B, and eleven organic impurities were identified in MDMA synthesised via Routes 2A and 2B.