Lancastergillespie4208

Increasing resistance to presently available antimalarial drugs urges the need to look for new promising compounds. The β-carboline moiety, present in several biologically active natural products and drugs, is an important scaffold for antimalarial drug discovery. The present study explores the antimalarial activity of a β-carboline derivative (1R,3S)-methyl 1-(benzo[d][1,3]dioxol-5-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate (9a) alone in vitro against Plasmodium falciparum and in vivo in combination therapy with the standard drug artesunate against Plasmodium berghei. Compound 9a inhibited both 3D7 and RKL-9 strains of P. falciparum with half-maximal inhibitory concentration (IC50) 10 against both the strains. The compound exhibited considerable in vivo antimalarial activity (median effective dose (ED50) = 27.74 mg/kg) in monotherapy. The combination of 9a (100 mg/kg) and artesunate (50 mg/kg) resulted in 99.69% chemosuppression on day 5 along with a mean survival time of 25.8 ± 4.91 days with complete parasite clearance. Biochemical studies indicated the safety of the HIT compound to hepatic and renal functions of mice. Molecular docking also highlighted the suitability of 9a as a potential antimalarial candidate.MXenes are the class of two-dimensional transition metal carbides and nitrides that exhibit unique properties and are used in a multitude of applications such as biosensors, water purification, electromagnetic interference shielding, electrocatalysis, supercapacitors, and so forth. Carbide-based MXenes are being widely explored, whereas investigations on nitride-based ones are seldom. Among the nitride-based MXenes obtained from their MAX phases, only Ti4N3 and Ti2N are reported so far. Herein, we report a novel synthesis of V2NT x (T x is the surface termination) obtained by the selective removal of "Al" from V2AlN by immersing powders of V2AlN in the LiF-HCl mixture (salt-acid etching) followed by sonication to obtain V2NT x (T x = -F, -O) MXene which is then delaminated using the dimethyl sulfoxide solvent. The V2NT x MXene is characterized by X-ray diffraction studies, field emission scanning electron microscope imaging, energy-dispersive X-ray spectroscopy, X-ray photoelectron spectroscopy, and high-resolution transmission electron microscope imaging. selleck kinase inhibitor Supercapacitor electrodes are prepared using V2NT x MXenes and their electrochemical performances are examined by cyclic voltammetry, galvanostatic charge/discharge measurement, and electrochemical impedance spectroscopy. The V2NT x MXene electrode exhibits a specific capacitance of 112.8 F/g at a current density of 1.85 mA/cm2 with an energy and power density of 15.66 W h/kg and 3748.4 W/kg, respectively, in 3.5 M KOH aqueous electrolyte. The electrode exhibits an excellent capacitance retention of 96% even after 10,000 charge/discharge cycles. An asymmetric supercapacitor fabricated with V2NT x as a negative electrode and Mn3O4 nanowalls as a positive electrode helps obtain a cell voltage of 1.8 V in aqueous KOH electrolyte.A new class of benzothiazole-appended quinoline derivatives (6-8) was synthesized via one-pot TPGS micellar-mediated acid-catalyzed nucleophilic addition, followed by aerobic oxidative cyclization of 3-formylquinoline-2-one (2), 3-formylquinoline-2-thione (3), and 2-azidoquinoline-3-carbaldehyde (4) individually with 2-amino thiophenol (5). The structures of the prepared compounds were confirmed using suitable spectroscopic methods complemented with single-crystal X-ray diffraction analysis. Time-dependent density functional theory-based optimization of molecular structures, bond lengths, bond angles, HOMO-LUMO energy gaps, and molecular electrostatic potential maps was theoretically computed at the B3LYP/6-311++g(d) level. The molecular docking studies recommended that 6-8 bound to the active site cavity of CD81 effectively with the binding energies of -6.9, -6.3, and -6.5 kcal mol-1, respectively. Further, MD simulation studies of compound 6 suggested that the binding resulted in the stabilization of the CD81 molecule. Thus, all theoretical predictions associated with the experimental verifications motivated to discover novel approaches for cancer therapy.Halloysite nanotubes (HNTs) have attracted great attention in the field of nanotechnology as natural, high value-added nanomaterials. Despite their significant potential as carriers of active agents and fillers in nanocomposite structures, inhomogeneity of HNTs in terms of length and diameter along with their agglomeration tendency poses important obstacles for the utilization of them in a wider range of applications. Here, a facile, three-step separation protocol that allows the sorting of HNTs into agglomeration-free, uniform size fractions is reported. The protocol consists of coating of HNTs with polydopamine to impart hydrophilicity and aqueous dispersibility, followed by their ultrasonication and centrifugation at varying velocities for size-based separation. Particle size distribution analysis by scanning electron microscopy and dynamic light scattering has demonstrated that the separation protocol resulted in uniform HNT fractions of varying agglomeration states and particle sizes. The highest qualityalities required by different applications can be selected.Synergistic use of superabsorbent hydrogels has vital contribution to the daily life. This work gives an account of a facile approach to synthesize superabsorbent hydrogels based on Moringa oleifera gum and polyvinyl alcohol cross-linked with borax. Fourier transform infrared, X-ray diffraction, and scanning electron microscopy were employed to characterize the structure, crystallinity, and surface morphologies of the samples. The cross-link density, swelling ratio, reswelling, water retention properties, and salt sensitivity of hydrogels were investigated. Reaction parameters for the hydrogel synthesis were optimized on the basis of water absorbency, and the reaction condition of greater water absorbency after 12 h at room temperature was taken as an ideal condition. Optimum conditions were obtained as [poly(vinyl alcohol) PVA] = 10% (w/v) and [borax] = 1.05 × 10-3 mol/L. Under the optimized conditions, the maximum swelling ratio of MOG/PVA hydrogel reached 1163 g/g in deionized water and 290 g/g in 0.9 wt % NaCl solution.