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Competing Interests: There are no conflicts of interest.

This study explored the impact of structural modifications on truncated 4'-selenonucleosides as ligands for the A 3 adenosine receptor (AR). We synthesized and evaluated a series of these compounds for their binding affinities, functional activities, and structural interactions by using computational modeling. The SAR study revealed that all compounds exhibited selective and notable hA 3 AR binding, among which 6l ( K i = 5.2 nM) and 6m ( K i = 5.7 nM) were found as the best binding compounds. The representative N 6 -cyclopropyl compound 6m was found to be a partial agonist, contrasting with the antagonist profiles of truncated 4'-oxo and 4'-thionucleosides. Computational docking highlighted 6m 's unique interaction with Thr94 at the A 3 AR binding site. This research not only advances our understanding of A 3 AR ligand interactions but also highlights the potential of truncated 4'-selenonucleosides as effective A 3 AR modulators., Competing Interests: The authors declare no competing financial interest., (© 2024 American Chemical Society.)

Iron oxide nanoparticles (IONPs) exhibit unique magnetic properties and possess a high surface-to-volume ratio, making them ideal candidates for the conjugation of substances, including enzymes. Laccase (EC 1.10.3.2), an oxidative enzyme with diverse applications, presents an opportunity for enhancing stability and reusability through innovative immobilization techniques, thus reducing overall process costs. In this study, we employed a direct binding procedure via carbodiimide activation to conjugate laccase onto IONPs synthesized using thermal chemical coprecipitation. Stabilization of the nanoparticles was achieved using thioglycerol and polyvinyl alcohol (PVA) as capping agents. Characterization of the synthesized nanoparticles was conducted using UV-spectroscopy, Fourier transform infrared spectroscopy (FTIR), x-ray diffraction, scanning electron microscopy, and energy dispersive x-ray spectroscopy. FTIR spectroscopy analysis confirmed successful laccase binding to magnetic nanoparticles, with binding efficiencies of 90.65% and 73.02% observed for thioglycerol and PVA capped IONPs, respectively. Furthermore, the conjugated enzyme exhibited remarkable stability, retaining nearly 50% of its initial activity after 20 reuse cycles. This research demonstrates that immobilizing laccase onto IONPs enhances its activity, stability, and reusability, with the potential for significant cost savings and expanded applications in various fields., (© 2024 IOP Publishing Ltd.)

Competing Interests: There are no conflicts of interest.

Introduction: The aim of the study was to evaluate the efficacy and safety of fixed-dose combination (FDC) of metoprolol, telmisartan, and chlorthalidone in patients with essential hypertension and stable coronary artery disease (CAD) who showed inadequate response to dual therapy., Methods: In this phase III, open-label, multicenter study, 254 adults with stable CAD having uncontrolled hypertension despite being treated with FDC of metoprolol (25/50 mg) and telmisartan (40 mg) were included. Patients received either of the following FDC for 24 weeks: metoprolol (25 mg), telmisartan (40 mg), and chlorthalidone (12.5 mg) (FDC1; n = 139) or metoprolol (50 mg), telmisartan (40 mg), and chlorthalidone (12.5 mg) (FDC2; n = 115) tablets once daily. The FDCs were developed using the novel Wrap Matrix™ platform technology. Primary endpoint assessed the mean change in seated diastolic blood pressure (SeDBP) and seated systolic blood pressure (SeSBP) from baseline to 24 weeks. Secondary efficacy endpoints included proportion of patients achieving < 90 mmHg SeDBP (SeDBP responder) and < 140 mmHg SeSBP (SeSBP responder) at weeks 12, 16, 20, and 24. Safety was assessed throughout the study., Results: A total of 243 (95.70%) patients completed study. The mean change in BP from baseline (FDC1, 155/96 mmHg; FDC2, 165/98 mmHg) to week 24 (FDC1, 128/82 mmHg; FDC2, 131/83 mmHg) was statistically significant (both groups p < 0.0001). Within FDC1 and FDC2, the mean change from baseline to week 24 in SeDBP (82.60 mmHg and 83.09 mmHg) and SeSBP (128.07 mmHg and 131.29 mmHg) was statistically significant (both groups p < 0.0001). At week 24, in FDC1, 80.15% and 84.73% were SeDBP and SeSBP responders, respectively; in FDC2, 79.46% and 74.11% were SeDBP and SeSBP responders, respectively. No serious adverse events or deaths were reported., Conclusion: Triple FDCs of metoprolol, telmisartan, and chlorthalidone were considered effective and well tolerated in patients with hypertension who respond inadequately to dual therapy., Clinical Trial Registration: CTRI/2016/11/007491., (© 2021. The Author(s), under exclusive licence to Springer Healthcare Ltd., part of Springer Nature.)

Heterocycles are the main structural motif of DNA and RNA and play a crucial role in various chemical reactions of metabolisms. Therefore, heterocyclic compounds show good physiological and pharmacological properties. Coumarin and pyrazole scaffolds are present in many commercial drug molecules and natural products. This review overviews the progress made in the synthesis and functionalization of the coumarin- pyrazole hybrid heterocycle. It also includes discussion on the possible reactive sites of heterocycles, functionalization, and mechanistic pathways to incorporate pyrazole pharmacophore unit in synthesis. Several synthesis and biological studies reveal that the combination of the coumarin-pyrazole moiety is a prominent structural motif to find lead compounds in drug discovery., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Thermoelectric (TE) materials are possible solutions of the current problems in the energy sector to overcome environmental pollution, increasing energy demand and the decline of natural resources. Thermoelectric materials are a promising alternative for the conversion of waste heat to electricity. Nanocrystalline PbTe powder was synthesized by a simple chemical method at room temperature and systematically investigated at various durations as samples A1-A5. Fourier Transform infrared spectroscopy (FTIR), x-ray diffraction (XRD), microstructural analysis by scanning electron microscopy (SEM), and energy dispersive spectroscopy (EDS) confirmed the composition of the samples. TE parameters as thermo-emf of samples A1-A5 and electrical conductivity were measured. The cyclic voltammetry gives a band gap of 0.25 eV, which is in agreement with the optical band gap of the material. The A4 sample has an average crystal size of 36 nm with preferred orientation in (200) verifying the cubic morphology. The obtained TE parameters are beneficial for the non-uniform TE materials which might be due to strong current boundary scattering and extremely low thermal conductivity of the samples.

A new method is developed to determine the presence of sunflower oil in olive oil. α-tocopherol is selected as discriminating parameter for detecting sunflower oil adulterant in olive oil. Admixtures of olive oil and sunflower oil (5 %, 10 %, 15 % and 20 % sunflower oil in olive oil) are prepared. These admixtures are analysed by reversed phase high pressure liquid chromatography coupled with fluorescence detector. The sample preparation does not require saponification or addition of antioxidant. The chromatographic system consists of a C18 column with methanol: acetonitrile (50:50) mobile phase. Fluorescence detector excitation wavelength is set at 290 nm and emission wavelength is set at 330 nm. The α tocopherol concentration increases linearly in olive oil adulterated with sunflower oil. The method is simple, selective, sensitive and is precise (RSD = 2.65 %) for α tocopherol. The present method can precisely detect 5 % sunflower oil in olive oil.

Nanostructured SnO2 thin films were prepared by spray pyrolysis technique onto glass substrates with different thickness by varying quantity of precursor solution. The structural, optical and electrical properties of these films have been studied. The crystallographic structure of the films was studied by X-ray diffraction (XRD). It is found that the films are tetragonal with (110) orientation. The grain size increases with thickness. Atomic Force Microscopy (AFM) showed that the nanocrystalline nature of the films with porous nature. The grain size increased 14 to 29 nm with increase in film thickness. The studies on the optical properties show that the direct band gap value decreases from 3.75 to 3.50 eV. The temperature dependence of the electrical conductivity was studied. The activation energies of the films are calculated from the conductance temperature characteristics. The nanostructured SnO2 thin films were used as sensing layers for resistive gas sensors. The dependence of gas sensing properties on the thickness of SnO2 thin films was investigated. The gas response of the SnO2 thin films towards the H2S gas was determined at an operating temperature of 150 degrees C. The sensitivity towards H2S gas is strongly depending on surface morphology of the SnO2 thin films.