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The New Delhi Metallo-β-lactamase-1 (NDM-1) causes hydrolysis of broad spectrum β-lactam antibiotics, such as carbapenems, resulting in the development of antimicrobial resistance. Still, there are not any approved NDM-1 inhibitors, globally. Therefore, repositioning approved medicines as NDM-1 inhibitors to combine with carbapenems may be a crucial strategy to combat resistant pathogens. This study repurposes. Oxicam derivatives as inhibitors of bacterial NDM-1. The two-dimensional structures were obtained from the PubChem database. Twenty derivatives of oxicam were assessed computationally to realize their NDM-1 inhibition capability. To identify potential inhibitors of the NDM-1 target protein, a molecular docking protocol was used. In addition, drug-likeness and pharmacokinetic properties were predicted for the designed molecules. Three compounds with the most negative ΔGbinding results were chosen for additional study using molecular dynamic (MD) simulations. The compounds M010, M013, and M016 possessed a significantly more negative binding free energy than the positive control and other designed molecules, had stable MD simulations (Root-mean-square deviation < 0.5 Å), passed Lipinski's rule of five, and possessed favourable physicochemical and pharmacokinetic properties. The findings can inform In vitro studies of the promising compounds.

In the classical approach to dealing with near-field radiative heat exchange between two closely spaced bodies, no coupling between the different heat carriers inside the materials and thermal photons is usually considered. Here, we provide an overview of the current state of research on this coupling between solids of different sizes while paying specific attention to the impact of the conduction regime inside the solids on the conduction–radiation coupling. We describe how the shape of the solids affects this coupling, and show that it can be located at the origin of a drastic change in the temperature profiles inside each body and the heat flux exchanged between them. These results could have important implications in the fields of nanoscale thermal management, near-field solid-state cooling, and nanoscale energy conversion.

Background: This is a single-centre prospective observational study examining radial access in 62 Prostatic Artery Embolisation (PAE) procedures. Evaluation of left radial artery diameter using high frequency ultrasound before and after administration of sublingual glycerl trinitrate (GTN). Pre-procedure questionnaires calculating symptom severity score compared with post-procedure. Results: Sublingual GTN resulted in a statistically significant increase in radial artery diameter (p <.00001). There was a statistically significant reduction in both average International Prostate Symptom Score (IPSS) and Quality of Life (QoL) from pre-procedure to post-PAE. The radial sheath was successfully inserted in 100% of cases. Crossover rate to femoral access was low (4%). Radial artery access had a low complication rate (2%). Radial artery variant anatomy was reasonably common (7%). Conclusions: Sublingual GTN significantly increase radial artery diameter. PAE from radial access is associated with a symptomatic improvement at 2-month follow-up. [ABSTRACT FROM AUTHOR]

Objective(s): Three physiological processes interact: sleep, learning, and stress. It is essential to understand how stress affects and interacts with the link between sleep, learning, and memory since it has long been recognized that sleep plays a crucial role in memory consolidation and learning. Through naloxone injection in the baso lateral amygdala (BLA), this study intends to shed light on the interactions between stress, learning, and sleep, as well as the function of the opioid system and its impact on brain-derived neurotrophic factor (BDNF) production in the hippocampus. Materials and Methods: Male Wistar rats (n=77) in eleven groups were implanted with electroencephalogram (EEG) and electromyography (EMG) recording electrodes, and the BLA area was bilaterally cannulated. Recordings of Rapid Eye Movement (REM) and Non-Rapid Eye Movement (NREM) sleep and wakefulness steps were made for the three hours prior to and three hours following the implementation of the immobility stress protocol and learning with the Barnes maze for three consecutive days. Also, the animals' memory was tasted 48 hr later. Before the stress and learning procedure, naloxone was injected into each BLA three times in a row at a dosage of 0.05 µg or 0.1 µg in a volume of 0.5 µl. A molecular biomarker of learning and stress, BDNF, was also examined. Results: The study demonstrated that the immobility stress model lowers REM and NREM sleep. On the other hand, putting the learning technique into practice results in more REM and NREM sleep, and stress situations do not stop this rise after learning. Naloxone injections in the BLA region also enhance learning and memory, preventing stress-related REM and NREM sleep loss. Additionally, stress lowers BDNF expression in the hippocampal region. BDNF expression rises in the hippocampus throughout the learning process, and naloxone administration in the BLA area also raises BDNF expression in the hippocampus. Conclusion: Stress generally reduces REM, NREM, and BDNF expression in the hippocampal region. Under stress, using the learning protocol increases REM, NREM sleep, and BDNF. Naloxone injection in BLA improves memory and learning, reducing stress-induced memory loss. [ABSTRACT FROM AUTHOR]

In the classical approach to dealing with near-field radiative heat exchange between two closely spaced bodies, no coupling between the different heat carriers inside the materials and thermal photons is usually considered. Here, we provide an overview of the current state of research on this coupling between solids of different sizes while paying specific attention to the impact of the conduction regime inside the solids on the conduction–radiation coupling. We describe how the shape of the solids affects this coupling, and show that it can be located at the origin of a drastic change in the temperature profiles inside each body and the heat flux exchanged between them. These results could have important implications in the fields of nanoscale thermal management, near-field solid-state cooling, and nanoscale energy conversion. [ABSTRACT FROM AUTHOR]

Alcohols and phenols were tetrahydropyranylated in the presence of H7[PMo8V4O40] in good to excellent yields in acetonitrile and under solventfree reaction conditions. A mild and convenient method for the formation and deprotection of tetrahydropyranyl ethers (THP ethers) is described. The formation of THP ethers from the corresponding alcohols was accomplished in the presence of acid-sensitive functional groups.