Convergent synthesis of carbonic anhydrase inhibiting bi-heterocyclic benzamides: Structure–activity relationship and mechanistic explorations through enzyme inhibition,kinetics, and computational studies

By using a convergent methodology, a novel series of N-arylated 4-yl-benzamides containing a bi-heterocyclic thiazole–triazole core was synthesized, and the structures of these hybrid molecules, 9a–k , were corroborated through spectral analyses. The in vitro studies of these multifunctional molecules demonstrated their potent carbonic anhydrase inhibition relative to the standard used. The kinetics mechanism was exposed by Lineweaver–Burk plots, which revealed that 9j inhibited carbonic anhydrase non-competitively by forming an enzyme-inhibitor complex. The inhibition constants K_i calculated from Dixon plots for this compound was 1.2 μM. The computational study was also persuasive with the experimental results, and these molecules disclosed good results of all scoring functions and interactions, which suggested a good binding to carbonic anhydrase. So, it was predicted from the inferred results that these molecules might be considered as promising medicinal scaffolds for various diseases related to the uncontrolled production of this enzyme.     

Aqueous‐Solution Route to Zinc Telluride Films for Application to CO2 Reduction

As a photocathode for CO₂ reduction, zinc‐blende zinc telluride (ZnTe) was directly formed on a Zn/ZnO nanowire substrate by a simple dissolution–recrystallization mechanism without any surfactant. With the most negative conduction‐band edge among p‐type semiconductors, this new photocatalyst showed efficient and stable CO formation in photoelectrochemical CO₂ reduction at ?0.2–?0.7 V versus RHE without a sacrificial reagent.     

PET Imaging of Bacterial Infections with Fluorine‐18‐Labeled Maltohexaose

A positron emission tomography (PET) tracer composed of ¹⁸F‐labeled maltohexaose (MH¹⁸F) can image bacteria in vivo with a sensitivity and specificity that are orders of magnitude higher than those of fluorodeoxyglucose (¹⁸FDG). MH¹⁸F can detect early‐stage infections composed of as few as 10⁵ E. coli colony‐forming units (CFUs), and can identify drug resistance in bacteria in vivo. MH¹⁸F has the potential to improve the diagnosis of bacterial infections given its unique combination of high specificity and sensitivity for bacteria.     

Surface-Plasmonic-Field-Induced Photoredox Catalysis and Mediated Electron Transfer for Washing-Free DNA Detection

Distance-dependent electromagnetic radiation and electron transfer have been commonly employed in washing-free fluorescence and electrochemical bioassays, respectively. In this study, we combined the two distance-dependent phenomena for sensitive washing-free DNA detection. A distance-dependent surface plasmonic field induces rapid photoredox catalysis of surface-bound catalytic labels, and distance-dependent mediated electron transfer allows for rapid electron transfer from the surface-bound labels to the electrode. An optimal system consists of a chemically reversible acceptor (Ru(NH₃)₆³⁺), a chemically reversible photoredox catalyst (eosin Y), and a chemically irreversible donor (triethanolamine). Side reactions with O₂ do not significantly decrease the efficiency of photoredox catalysis. Energy transfer quenching between the electrode and the label can be lowered by increasing the distance between them. Washing-free DNA detection had a detection limit of approximately 0.3 nm in buffer and 0.4 nm in serum without a washing step.     

Stress variations during polarization of iron thin film electrode in pH 8.4 borate buffer solution

Journal of Solid State Electrochemistry - The stress variations during polarization of iron thin film electrode in pH 8.4 borate buffer solution have been measured by a cantilever bending...     

γ‐Glutamylcysteine‐ and Cysteinylglycine‐Directed Growth of Chiral Gold Nanoparticles and their Crystallographic Analysis

Chiral optical metamaterials with delicate structures are in high demand in various fields because of their strong light–matter interactions. Recently, a scalable strategy for the synthesis of chiral plasmonic nanoparticles (NPs) using amino acids and peptides has been reported. Reported herein, 3D chiral gold NPs were synthesized using dipeptide γ‐Glu‐Cys and Cys‐Gly and analyzed crystallographically. The γ‐Glu‐Cys‐directed NPs present a cube‐like outline with a protruding chiral wing. In comparison, the NPs synthesized with Cys‐Gly exhibited a rhombic dodecahedron‐like outline with curved edges and elliptical cavities on each face. Morphology analysis of intermediates indicated that γ‐Glu‐Cys generated an intermediate concave hexoctahedron morphology, while Cys‐Gly formed a concave rhombic dodecahedron. NPs synthesized with Cys‐Gly are named 432 helicoid V because of their unique morphology and growth pathway.     

Influence of the dispersed phase upon the behaviour of nylon/rubber blends; crosslinking effect

Nylon 6 and crosslinked SBS rubber blends were prepared. Their impact strength tests demonstrated the possibility of the existence of a maximum in impact strength at a moderate degree of crosslinking level. However, its peak value was not so much eminent as that happened in tensile test or brittle polymer's impact test. This seems due to complex mechanism occurred in dispersed phase. Based on our experimental data, we believe cavitation is important in nylon toughening. Interpretation of nylon toughening mechanism by cavitation and particle deformation is suggested for the reason of low peak value. Even though delamination is also possible, tensile strength data support cavitation in the rubber particle which seems to be more plausible for toughened nylon 6.     

Analysis of phantom centering positioning on image noise and radiation dose in axial scan type of brain CT

ABSTRACT

This study examined the dose and image quality according to the position change of a human phantom in a CT scan. This study used an MDCT 128 Slice CT Scanner instrument. An axial scan was performed with a 16 cm CTDI phantom of a human phantom, and the dose was measured using a pencil chamber meter. The phantom was scanned 10 cm above and below the isocenter and 15 cm above the right and left. The position of the phantom is indicated by C-0 in the isocenter position, S-10 in the upper 10 cm, I-10 in the lower 10 cm, R-15 in the right 15 cm, and L-15 in the left 15 cm. The test was performed 30 times using the brain CT protocol to calculate the dose and the dose width product (DWP). The acquired images were analyzed using the ImageJ program. Statistical analysis was performed using SPSS with one-way ANOVA (p < .05). The mean DWP values of the CT scanner were C-0 31.97 mGy·cm, S-10 24.52 mGy·cm, I-10 24.28 mGy· cm, R-15 17.95 mGy·cm, and L15 17.6 mGy·cm. Compared to the isocenter (C-0), the DLP values measured at each site were 23.3% for S-10, 24% for I-10, 43.8% for R-15, and 44.9% for L15. A significant difference in the one-way ANOVA statistical process was observed (p>0.05). C-0 was measured to be 7.42 HU, S-10 7.87 HU, I-10 8.4 HU, R-15 117 HU, and L-15 13.6 HU for evaluating the image quality. Compared to C-0, S-10 was 5.39%, I-10 was 13.2%, R-15 was 57.6%, and L-15 was 83.2%. The PSNR for S-10, I-10, R-15, and L-15 was 17.37, 17.5, 16.62, and 16.37 dB, respectively. A good quality image can be obtained by positioning the subject precisely in the isocenter in the axial scan, if possible, because the irradiated dose to the subject is low, which can lead to an increase in noise in image reconstruction.     

Preparation and characterization of self-assembled nanoparticles based on glycol chitosan bearing adriamycin

An anthracycline drug, adriamycin, was chemically conjugated onto the backbone of glycol chitosan via an acid-labile cis-aconityl linkage. The physicochemical characteristics of the glycol chitosan–adriamycin (GC–ADR) conjugates were investigated by dynamic light scattering, atomic force microscopy, and fluorescence spectroscopy. The GC–ADR conjugates were capable of forming nano-sized self-aggregates in an aqueous medium, when the adriamycin content in the conjugate was in the range of 2.0–5.0 wt.%. The self-aggregates were spherical in shape, and had mean diameters of 238–304 nm, depending on the adriamycin content. The critical aggregation concentrations of the conjugates, estimated by the fluorescence quenching method, were as low as 1.0–2.5×10⁻² mg/ml. The size of self-aggregates was not affected by the polymer concentration in the range from 50 to 2,000 μg/ml, and was maintained up to 8 days in phosphate-buffered saline (pH 7.4), indicating high colloidal stability. The release of adriamycin from self-aggregates was significantly dependent on the pH of the medium due to the cis-aconityl linkage; e.g., the amount of adriamycin released for 4 days was 7.3±0.3% at pH 7, whereas it was 29.3±1.9% at pH 4. The cell viability results demonstrated that free adriamycin shows more potent cytotoxicity than the conjugates, primarily attributed to the sustained release of adriamycin from self-aggregates. In conclusion, the self-aggregates, formed by GC–ADR conjugates, might be useful for the site-specific delivery of adriamycin in a sustained manner.