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The first zinc(II)-catalyzed approach towards an array of 2-aminobenzothiazole derivatives was successfully developed. In this process, the substrate 2-bromophenyl isothiocyanate was reacted with a range of amines, including aromatic and aliphatic (primary and secondary) and cyclic secondary amines, yielding the products in reasonably good amounts. The reactivity analyses of different amines revealed that cyclic secondary amines performed exceptionally well, providing excellent outcomes. Additionally, aliphatic amines also exhibited the capability to undergo the transformation successfully.

CO.sub.2 regeneration and reutilization is considered to be a green and effective route with highly potential for development. CeO.sub.2 showed high catalytic activity for the production of N,N'-dibutylurea through n-butyl amine and CO.sub.2. Herein, V-doped CeO.sub.2 with different molar ratios of V/Ce (V.sub.x%-CeO.sub.2, x = 0, 0.4, 0.6, 0.8 and 1.0) were further successfully synthesized and firstly applied to the reaction of CO.sub.2 with n-butyl amine. The reaction results displayed the catalytic performance of CeO.sub.2 were prominently enhanced by doping V.sup.5+ and followed an order of V.sub.0.8%-CeO.sub.2 > V.sub.0.6%-CeO.sub.2 > V.sub.1.0%-CeO.sub.2 > V.sub.0.4%-CeO.sub.2 > CeO.sub.2. The reason for the changes in the catalytic activities of CeO.sub.2 with different doping amounts of V.sup.5+ could be closely related to the surface oxygen vacancy and surface weak acidity and weak basicity based on specific analysis of relevant characterization including XRD, BET, Raman, XPS, EPR and NH.sub.3/CO.sub.2-TPD.

The synthesis of stereochemically pure oximes, amines, saturated and unsaturated cyanomethyl compounds, and methylaminomethyl compounds at the C9 position in 3-hydroxy-N-phenethyl-5-phenylmorphans provided μ-opioid receptor (MOR) agonists with varied efficacy and potency. One of the most interesting compounds, (2-((1S,5R,9R)-5-(3-hydroxyphenyl)-2-phenethyl-2-azabicyclo[3.3.1]nonan-9-yl)acetonitrile), was found to be a potent partial MOR agonist (EC[sub.50] = 2.5 nM, %E[sub.max] = 89.6%), as determined in the forskolin-induced cAMP accumulation assay. Others ranged in potency and efficacy at the MOR, from nanomolar potency with a C9 cyanomethyl compound (EC[sub.50] = 0.85 nM) to its totally inactive diastereomer, and three compounds exhibited weak MOR antagonist activity (the primary amine 3, the secondary amine 8, and the cyanomethyl compound 41). Many of the compounds were fully efficacious; their efficacy and potency were affected by both the stereochemistry of the molecule and the specific C9 substituent. Most of the MOR agonists were selective in their receptor interactions, and only a few had δ-opioid receptor (DOR) or κ-opioid receptor (KOR) agonist activity. Only one compound, a C9-methylaminomethyl-substituted phenylmorphan, was moderately potent and fully efficacious as a KOR agonist (KOR EC[sub.50] = 18 nM (% E[sub.max] = 103%)).

The acylation of amines has always attracted a deep interest as a synthetic route due to its high versatility in organic chemistry and biochemical processes. The purpose of this article is to present a mechanochemical acylation procedure based on the use of acyl-saccharin derivatives, namely N-formylsaccharin, N-acetylsaccharin, and N-propionylsaccharin. This protocol furnishes a valuable solvent-free alternative to the existing processes and aims to be highly beneficial in multi-step procedures due to its rapid and user-friendly workup.

In this study, we outline the eco-friendly mechanosynthesis of N-(2,2-diphenylethyl)-4-nitrobenzamide by reacting 2,2-diphenylethan-1-amine with 4-nitrobenzoyl chloride. The resulting bio-functional hybrid compound was meticulously characterized through the analysis of [sup.1]H-, [sup.13]C-NMR, UV, and detailed mass spectral analysis.

In the quest for net zero carbon emissions by 2050, Carbon Capture Utilization and Storage (CCUS) is indispensable. The development of more efficient CO[sub.2] capture processes is essential. High-frequency ultrasonic irradiation is an emerging, intensified technique that can enhance the CO[sub.2] absorption process. To advance this technology toward commercialization, it is crucial to conduct a thorough economic analysis to allow the identification of the key cost component. While equipment sizing is essential in this economic assessment, there is a lack of numerical models for estimating the size and power consumption of ultrasonic absorbers. This study introduces a numerical model for these predictions. The model was then used to determine the economic feasibility of this emerging technique against the packed bed columns based on capital expenditure (CAPEX), operational expenditure (OPEX), and unit technical cost (UTC) for 20 years of plant operation. According to the economic analysis, ultrasonic intensification requires 34% less CAPEX due to its compact design. Although its OPEX is 11% higher due to the additional electricity needed for the ultrasonic transducers, the UTC is still 3% lower than the conventional packed bed column, demonstrating a potential cost savings in implementing the ultrasonic irradiation-assisted technique during the CO[sub.2] absorption process offshore.

Odorants are detected as smell in the nasal epithelium of mammals by two G-protein-coupled receptor families, the odorant receptors and the trace amine-associated receptors 1 , 2 (TAARs). TAARs emerged following the divergence of jawed and jawless fish, and comprise a large monophyletic family of receptors that recognize volatile amine odorants to elicit both intraspecific and interspecific innate behaviours such as attraction and aversion 3 – 5 . Here we report cryo-electron microscopy structures of mouse TAAR9 (mTAAR9) and mTAAR9–G s or mTAAR9–G olf trimers in complex with β-phenylethylamine, N , N -dimethylcyclohexylamine or spermidine. The mTAAR9 structures contain a deep and tight ligand-binding pocket decorated with a conserved D 3.32 W 6.48 Y 7.43 motif, which is essential for amine odorant recognition. In the mTAAR9 structure, a unique disulfide bond connecting the N terminus to ECL2 is required for agonist-induced receptor activation. We identify key structural motifs of TAAR family members for detecting monoamines and polyamines and the shared sequence of different TAAR members that are responsible for recognition of the same odour chemical. We elucidate the molecular basis of mTAAR9 coupling to G s and G olf by structural characterization and mutational analysis. Collectively, our results provide a structural basis for odorant detection, receptor activation and G olf coupling of an amine olfactory receptor. Cryo-electron microscopy structures of mouse trace amine-associated receptor 9 reveals structural motifs involved in odorant ligand recognition, including a unique disulfide bond linking the N terminus to extracellular loop 2.

Refractory chronic cough causes substantial symptoms and quality-of-life impairment. Similarities between central reflex sensitisation in refractory chronic cough and neuropathic pain suggest that neuromodulators such as gabapentin might be effective for refractory chronic cough. We established the efficacy of gabapentin in patients with refractory chronic cough. This randomised, double-blind, placebo-controlled trial was undertaken at an outpatient clinic in Australia. Adults with refractory chronic cough (>8 weeks' duration) without active respiratory disease or infection were randomly assigned to receive gabapentin (maximum tolerable daily dose of 1800 mg) or matching placebo for 10 weeks. Block randomisation was done with randomisation generator software, stratified by sex. Patients and investigators were masked to assigned treatment. The primary endpoint was change in cough-specific quality of life (Leicester cough questionnaire [LCQ] score) from baseline to 8 weeks of treatment, analysed by intention to treat. This study is registered with the Australian New Zealand Clinical Trials Registry, number ACTRN12608000248369. 62 patients were randomly assigned to gabepentin (n=32) or placebo (n=30) and ten patients withdrew before the study end. Gabapentin significantly improved cough-specific quality of life compared with placebo (between-group difference in LCQ score during treatment period 1·80, 95% CI 0·56–3·04; p=0·004; number needed to treat of 3·58). Side-effects occurred in ten patients (31%) given gabapentin (the most common being nausea and fatigue) and three (10%) given placebo. The treatment of refractory chronic cough with gabapentin is both effective and well tolerated. These positive effects suggest that central reflex sensitisation is a relevant mechanism in refractory chronic cough. National Health and Medical Research Council of Australia and Hunter Medical Research Institute, Newcastle, Australia.

This work is focused on the application of lanthanide-free perovskite Ba[sub.1−x]Sr[sub.x]TiO[sub.3] (0 < x < 1) in valorization of toxic pollutants as 4-nitrophenol (4-NPh). The series of perovskites were fabricated by facile, one-step solid-state preparation method and characterized via various techniques: elemental analysis (Inductively Coupled Plasma Optical Emission Spectrometry, ICP-OES), powder X-ray diffraction (XRD), scanning electron microscopy (SEM), Fourier-transform infrared spectroscopy (FTIR) and dielectric properties (impedance spectroscopy, IS). The methods confirmed the assumed composition, structure and high purity of the materials. The results showed that substitution of Ba[sup.2+] by Sr[sup.2+] in the perovskite crystal lattice influenced the dielectric properties of samples and the size of the grains. The absorption and catalytic properties of Ba[sub.(1−x)]Sr[sub.x]TiO[sub.3] (0 < x < 1) series were evaluated in reduction of 4-NPh in water using NaBH[sub.4] as reducing agent. No adsorption of 4-NPh was found for all the materials during 180 min of contact (experiment without reducing agent), and the best catalytic performance was found for the Ba[sub.(1−x)]Sr[sub.x]TiO[sub.3] (x = 0.3) sample. The catalytic transformation of 4-NPh to 4-APh follows a pseudo-first-order model, and the catalysts can be easily regenerated via mild annealing (300 °C).

Many central nervous system disorders (CNS), including chronic pain and migraine, involve metabolic changes in the brain. These changes are best detected and monitored in cerebrospinal fluid (CSF), which requires lumbar puncture. Blood-based measurements may offer an alternative, if they reflect CSF changes. To assess this, we measured and correlated the concentrations of 39 amino acids, biogenic amines, and other amines in blood and CSF of 95 healthy volunteers and, in addition, correlated the ratios of 741 amines. Amines were measured using a validated UPLC-MS platform. In healthy volunteers, only 4/39 (10.3%) analyzed amine metabolite concentrations had a correlation coefficient ≥ 0.70. Correlations of metabolite ratios were significantly better for 308/741 (41.5%) combinations. Specifically, ratios of amino acids showed high correlations. In addition, amines were investigated in 197 participants with migraine. Six amine metabolite ratios were different in migraineurs versus healthy volunteers. Most blood amine concentrations do not reflect those in CSF, but many of the ratios did correlate between CSF and plasma, showing diagnostic potential. This study improves our understanding of blood-CSF relationships, and our data suggest that ratios of amines may be of relevance to CNS disorders, as we showed for migraine.