High Yielding Synthesis of Carboranes Under Mild Reaction Conditions Using a Homogeneous Silver(I) Catalyst: Direct Evidence of a Bimetallic Intermediate

Methods used to prepare functionalized carboranes generally require heating to high temperatures, and thus limits the range of derivatives which can be prepared directly from alkynes. We show here that by using a homogeneous silver(I) catalyst it is now possible to prepare carboranes in good to excellent yield at temperatures below 40 °C, including at room temperature. The process is general and provides an important new synthetic strategy for the preparation of functionalized boron clusters.     

Pest management of two non-interacting pests in presence of common predator

The paper considers two mutually independent pests in presence of their common predator and discusses their control biologically by release of additional predators and chemically by using non-selective non-residual pesticide. It also verifies the results by special choice of parameters.     

Analyzing fragment production in mass-asymmetric reactions as a function of density dependent part of symmetry energy

We performed a theoretical investigation of different mass-asymmetric reactions to access the direct impact of the density-dependent part of symmetry energy on multifragmentation. The simulations are performed for a specific set of reactions having same system mass and N/Z content, using isospin-dependent quantum molecular dynamics model to estimate the quantitative dependence of fragment production on themass-asymmetry factor (τ) for various symmetry energy forms. The dynamics associated with different mass-asymmetric reactions is explored and the direct role of symmetry energy is checked. Also a comparison with the experimental data (asymmetric reaction) is presented for a different equation of states (symmetry energy forms).     

Urea derivatives of piperazine doped with pyrazole-4-carboxylic acids: Synthesis and antimicrobial evaluation

A series of novel N-cycloalkyl/aryl-4-(1,3-diphenyl-1H-pyrazole-4-carbonyl)piperazine-1-carboxamides 9a-g has been synthesized for biological interest by simple base catalyzed reaction of various N-cycloalkyl/aryl isocyanates with (1,3-diphenyl-1H-pyrazol-4-yl)(piperazin-1-yl)methanone hydrochloride 8 . The compound 8 was synthesized in excellent yield by the reaction of 1,3-diphenyl-1H-pyrazole-4-carbonyl chloride with boc-piperazine followed by deprotection of boc group with dioxane-HCl. All the novel intermediates and urea derivatives have been screened for antimicrobial activity. The compound 9a was found an excellent compound to be active against all Gram (−ve) and Gram (+ve) bacterial strains E. coli, Y. enterocolitica, B. cereus, and S. aureus. It also showed comparable antifungal activity against C. albicans with MIC 78.1 μg/ml as compared to reference standard miconazole.     

Plasticizing effects of epoxidized sun flower oil on biodegradable polylactide films: A comparative study

Polylactide (PLA) is one of the most promising materials among the renewable source-based biodegradable plastics. However, high inherent stiffness and brittleness of the pure PLA is often insufficient for wide range of engineering applications. One of the best ways to improve the processability, toughness and flexibility of PLA is to plasticize with epoxidized plant oils. In this work, epoxidized sun flower oil (ESFO) was incorporated into PLA matrix. The thermal, mechanical, biodegradation, optical transmission properties and fracture morphology of ESFO plasticized PLA were investigated to make a comparison with that of PLA plasticized by commercial epoxidized soya bean oil (ESO). Results show that a remarkable improvement of elongation at break was observed in the case of ESFO incorporated PLA. Although a slightly decrease the T _g of PLA was resulted from the plasticizing effects of ESFO, the thermal stability of the plasticized PLA was improved. On the other hand, the ESFO plasticized PLA showed a higher level of UV adsorption but a lower level of biodegradation ratio. After all, ESFO exhibited similar effects on the biodegradable PLA films to ESO, which is anticipated to be a good candidate for plasticizing biodegradable polymer materials.     

Synthesis and characterization of high bio-based content unsaturated polyester resin for wood coating from itaconic acid: Effect of various reactive diluents as an alternative to styrene

The present work focuses on the ability of 2-hydroxyethyl methacrylate (HEMA), isobornyl methacrylate (IBOMA) and methyl methacrylate (MMA) as reactive diluents to replace styrene in unsaturated polyester resin based on itaconic acid, sebacic acid, 1,4-Butanediol, 1,6-Hexanediol and glycerol. The structural analysis confirmed the presence of itaconate linkages in the UPs. The synthesized resins were characterized by infrared spectroscopy and their physiochemical properties such as appearance, viscosity, acid value, %volatile content, curing characteristics like gel time, peak exotherm temperature and total cure time. Among all the resins formed; the resin based on 1,6-Hexanediol showed optimum molecular weight and viscosity needed for final application. The cured resins were investigated for their thermal stability by thermo-gravimetric analysis which revealed that all the diluted resins had good thermal stability. From the results it could be concluded that styrene-free bio-based unsaturated polyester resin can be synthesized having properties equivalent to the commercial styrene based resin.GRAPHICAL ABSTRACT     

A Fluorogenic Assay: Analysis of Chemical Modification of Lysine and Arginine to Control Proteolytic Activity of Trypsin

The chemical modification of amino acids plays an important role in the modulation of proteins or peptides and has useful applications in the activation and stabilization of enzymes, chemical biology, shotgun proteomics, and the production of peptide-based drugs. Although chemoselective modification of amino acids such as lysine and arginine via the insertion of respective chemical moieties as citraconic anhydride and phenyl glyoxal is important for achieving desired application objectives and has been extensively reported, the extent and chemoselectivity of the chemical modification of specific amino acids using specific chemical agents (blocking or modifying agents) has yet to be sufficiently clarified owing to a lack of suitable assay methodologies. In this study, we examined the utility of a fluorogenic assay method, based on a fluorogenic tripeptide substrate (FP-AA1-AA2-AA3) and the proteolytic enzyme trypsin, in determinations of the extent and chemoselectivity of the chemical modification of lysine or arginine. As substrates, we used two fluorogenic tripeptide probes, MeRho-Lys-Gly-Leu(Ac) (lysine-specific substrate) and MeRho-Arg-Gly-Leu(Ac) (arginine-specific substrate), which were designed, synthesized, and evaluated for chemoselective modification of specific amino acids (lysine and arginine) using the fluorogenic assay. The results are summarized in terms of half-maximal inhibitory concentrations (IC₅₀) for the extent of modification and ratios of IC₅₀ values (IC₅₀arginine/IC₅₀lysine and IC₅₀lysine/IC₅₀arginine) as a measure of the chemoselectivity of chemical modification for amino acids lysine and arginine. This novel fluorogenic assay was found to be rapid, precise, and reproducible for determinations of the extent and chemoselectivity of chemical modification.     

Thermal–electrical–structural performances of hot heat exchanger with different internal fins of thermoelectric generator for low power generation application

Journal of Thermal Analysis and Calorimetry - In this study, an electro-thermo-structural coupled numerical analysis is conducted to evaluate the thermal, electrical, and structural performances of...     

The HDAC/HSP90 Inhibitor G570 Attenuated Blue Light-Induced Cell Migration in RPE Cells and Neovascularization in Mice through Decreased VEGF Production

Age-related macular degeneration (AMD) occurs due to an abnormality of retinal pigment epithelium (RPE) cells that leads to gradual degeneration of the macula. Currently, AMD drug pipelines are endowed with limited options, and anti-VEGF agents stand as the dominantly employed therapy. Despite the proven efficacy of such agents, the evidenced side effects associated with their use underscore the need to elucidate other mechanisms involved and identify additional molecular targets for the sake of therapy improvement. The previous literature provided us with a solid rationale to preliminarily explore the potential of selective HDAC6 and HSP90 inhibitors to treat wet AMD. Rather than furnishing single-target agents (either HDAC6 or HSP90 inhibitor), this study recruited scaffolds endowed with the ability to concomitantly modulate both targets (HDAC6 and HSP90) for exploration. This plan was anticipated to accomplish the important goal of extracting amplified benefits via dual inhibition (HDAC6/HSP90) in wet AMD. As a result, G570 (indoline-based hydroxamate), a dual selective HDAC6-HSP90 inhibitor exerting its effects at micromolar concentrations, was pinpointed in the present endeavor to attenuate blue light-induced cell migration and retinal neovascularization by inhibiting VEGF production. In addition to the identification of a potential chemical tool (G570), the outcome of this study validates the candidate HDAC6-HSP90 as a compelling target for the development of futuristic therapeutics for wet AMD.