Characterization of activated biomass carbon from tea leaf for supercapacitor applications.

In this study, a facile synthesis of chemical and thermal activation of biomass tea-waste materials was explored. A tea-waste biosource carbon was explored by chemical vapor deposition (CVD) method at 700 °C. The KOH-treated carbon (AC-KH) and H3PO4-treated carbon (AC-HP) were systematically studied for morphological characteristics and showed good morphological structures and a few transparent focused layered nanosheets. The elemental analysis done by scanning electron microscopy with energy-dispersive X-ray spectroscopy confirmed the presence of activated carbon. Fourier transform infrared spectroscopy (FT-IR) showed carbon-containing functional groups. The electrochemical analysis showed cyclic voltammetry (CV) curves for electric double layer capacitance (EDLC) with 3 M KOH electrolyte. The Nyquist plot obtained using electrochemical impedance spectroscopy (EIS) showed charge transfer resistance value (Rct) of 6.08 Ω. The electrochemical galvanostatic charge-discharge (GCD) study was conducted to obtain the specific capacitance (Scp) values of AC-KH, which were found to be 131.95 F/g at 0.5 A/g and also AC-HP active material was observed 55.76 F/g at 1 A/g. The AC-KH showed superior electrochemical performance when compared to AC-HP material. Hence, AC-KH is a promising active material for high-energy supercapacitor applications.

Pure and Ce-doped spinel CuFe2O4 photocatalysts for efficient rhodamine B degradation.

Wastewater management is becoming a serious issue worldwide. To enhance the reuse of wastewater, one has to remove toxic pollutants present in it. High amount of dye is present in wastewater, and to remove these dyes is the large scope of this research. Herein, we report production of pure and Ce-doped copper ferrite via hydrothermal route. The synthesized nanoparticles were collected and analyzed by basic characterization techniques. The bandgap energy calculated for pure, 1% Ce, and 2% Ce-doped CuFe2O4 was found to be 2.77, 2.57, and 2.36eV, respectively. Reduction in bandgap was attributed to the doping element. The shape and size of pure and Ce-doped products were investigated using a scanning electron microscope. Agglomeration was observed in the pure copper ferrite sample. In the Ce-doped sample, agglomeration was clearly reduced and the 2% Ce-doped CuFe2O4 sample showed growth of small nanoparticles. They showed complete growth and were arranged in a uniform manner without agglomeration. The surface area of the 2% Ce-CuFe2O4 sample was found to be 65.89 m2/g with 7.02 nm pore diameter. The photocatalytic activity of the prepared material was observed for rhodamine B degradation. The pure and catalyst-added dye was exposed under visible light. The samples were tested for UV. The efficiency obtained for pure dye solution, pristine CuFe2O4-added, and 1% Ce and 2% Ce-doped CuFe2O4-added dye solutions were 48%, 50%, 66%, and 88% within 2 h of irradiation. The 2% Ce-doped CuFe2O4 sample showed excellent photocatalytic activity as the bandgap and morphology were enhanced by doping an appropriate ratio of Ce ions.

Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.

The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune diseases. A small molecule, inverse agonist of the receptor is anticipated to reduce production of IL-17, a key proinflammatory cytokine. Through a high-throughput screening approach, we identified a molecule displaying promising binding affinity for RORC2, inhibition of IL-17 production in Th17 cells, and selectivity against the related RORA and RORB receptor isoforms. Lead optimization to improve the potency and metabolic stability of this hit focused on two key design strategies, namely, iterative optimization driven by increasing lipophilic efficiency and structure-guided conformational restriction to achieve optimal ground state energetics and maximize receptor residence time. This approach successfully identified 3-cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide as a potent and selective RORC2 inverse agonist, demonstrating good metabolic stability, oral bioavailability, and the ability to reduce IL-17 levels and skin inflammation in a preclinical in vivo animal model upon oral administration.

Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.

Leucine rich repeat kinase 2 (LRRK2) has been genetically linked to Parkinson's disease (PD) by genome-wide association studies (GWAS). The most common LRRK2 mutation, G2019S, which is relatively rare in the total population, gives rise to increased kinase activity. As such, LRRK2 kinase inhibitors are potentially useful in the treatment of PD. We herein disclose the discovery and optimization of a novel series of potent LRRK2 inhibitors, focusing on improving kinome selectivity using a surrogate crystallography approach. This resulted in the identification of 14 (PF-06447475), a highly potent, brain penetrant and selective LRRK2 inhibitor which has been further profiled in in vivo safety and pharmacodynamic studies.

HIV and SIV induce alterations in CNS CaMKII expression and activation: a potential mechanism for cognitive impairment.

The molecular mechanisms underlying learning and memory impairment in patients with HIV-associated neurological disease have remained unclear. Calcium/calmodulin-dependent kinase II (CaMKII) has key roles in synaptic potentiation and memory storage in neurons and also may have immunomodulatory functions. To determine whether HIV and simian immunodeficiency virus (SIV) induce alterations in CaMKII expression and/or activation (autophosphorylation) in the brain, we measured CaMKII alterations by quantitative immunoblotting in both an in vitro HIV/neuronal culture model and in vivo in an SIV-infected macaque model of HIV-associated neurological damage. Using primary rat hippocampal neuronal cultures treated with culture supernatants harvested from HIV-1-infected human monocyte-derived macrophages (HIV/MDM), we found that CaMKII activation declined after exposure of neurons to HIV/MDM. Consistent with our in vitro measurements, a significant decrease in CaMKII activation was present in both the hippocampus and frontal cortex of SIV-infected macaques compared with uninfected animals. In SIV-infected animals, total CaMKII expression in the hippocampus correlated well with levels of synaptophysin. Furthermore, CaMKII expression in both the hippocampus and frontal cortex was inversely correlated with viral load in the brain. These findings suggest that alterations in CaMKII may compromise synaptic function in the early phases of chronic neurodegenerative processes induced by HIV.

Synthesis and purine receptor affinity of 6-oxopurine nucleosides and nucleotides containing (N)-methanocarba-pseudoribose rings.

6-Oxopurine derivatives containing a northern (N) methanocarba modification (i.e., fused cyclopropane and cyclopentane rings in place of the ribose) were synthesized and the adenosine receptor affinity measured. Guanine or hypoxanthine was coupled at the 7-position, or 1,3-dibutylxanthine was coupled at the 9-position. The pseudoribose ring was also substituted at the 5'-position with an N-methyluronamide or with phosphate groups.