A ligand free copper(II) catalyst is as effective as a ligand assisted Pd(II) catalyst towards intramolecular C–S bond formation via C–H functionalization

Copper(I) catalysts are usually ineffective on the other hand Pd(II) catalysts are quite effective in promoting intramolecular sp² C–H functionalization (C–S bond formation). Herein, we have developed a ligand assisted Pd(II) catalyzed C–S bond formation via C–H activation from arylthioureas leading to the formation of 2-aminobenzothiazoles for substrates bearing electron donating (EDG) groups in the aryl ring. However without the assistance of ligand this Pd(II) catalyzed reaction is quite unproductive particularly for thioureas possessing strongly electron donating groups in the aryl rings. Interestingly, the ligand free Cu(II) catalyzed oxidative cyclization of arylthioureas are equally effective both for arylthioureas possessing electron donating as well as electron withdrawing groups in the aryl rings.     

Heteropoly acid catalyzed synthesis of 8-methyl-2-aryl/alkyl-3-oxabicyclo[3.3.1]non-7-ene derivatives through (3,5)-oxonium-ene reaction

A variety of aldehydes undergo a smooth coupling with (4-methylcyclohex-3-en-1-yl)methanol in the presence of 2 mol % of phosphomolybdic acid in dichloromethane to afford 3-oxabicyclo[3.3.1]non-7-ene in good yields through 3,5-oxonium-ene cyclization under mild conditions. The use of inexpensive, nontoxic, and readily available heteropoly acid catalyst makes this method simple, convenient, and environmental-friendly.     

Realization of vibronic entanglement in terms of tunneling current in an artificial molecule

Based on the concept of molecular nonadiabatic processes, namely, curve crossing and electronic interstate coupling, here we have introduced a model of an artificial molecule composed of three coupled quantum dots in terms of displaced harmonic oscillators of the confinement potential. We have shown that the static and dynamic features of vibronic entanglement can be realized in terms of the tunneling current in our model. An entanglement sudden-death can be shown to be equivalent to the suppression of tunneling current at the appropriate parameters of the magnetic field. We have also provided the nonclassicality of the vibration of the dot confinement potential which maximizes at the anticrossing zone.     

Selective fluorescence and naked eye detection of histidine in aqueous medium via hydrogen bonding assisted Schiff base condensation

Visible light excitable rhodamine B derivative (TARDHD) has been developed for fluorescence and naked eye detection of histidine in aqueous medium. TARDHD shows 45 fold fluorescence enhancement in the presence of histidine. It forms Schiff base with histidine and stabilizes via intra-molecular H-bonding. TARDHD can efficiently detect intracellular histidine.     

Radiolabeled novel peptide for imaging somatostatin-receptor expressing tumor: synthesis and radiobiological evaluation

The aim of this study was to synthesis, a radiolabeled (^99mTc) new somatostatin-analogue 6-hydrazinopyridine-3-carboxylic-acid (HYNIC)-Asn³-octreotate (^99mTc-HYNIC-AATE), and to evaluate as a candidate for imaging somatostatin-receptor (SSTR)-positive tumors and also compare it with ^99mTc-HYNIC-Tyr³-octreotide (^99mTc-HYNIC-TOC). Synthesis was performed by Fmoc-solid-phase strategy and ^99mTc labeled by SnCl₂. Biodistribution and imaging properties of new radiopeptide were also studied in C6 tumor bearing rat. Radiolabeling was performed at high specific activities and it showed high binding-affinity for SSTR2. In biodistribution, radiopeptides have showed high and receptor-specific uptake in the SSTR2 positive organs, tumor with rapid renal excretion from non-target tissues. These results demonstrated that ^99mTc-HYNIC-AATE is a new specific radioligand for scintigraphy of somatostatin-receptor-positive tumors.     

High accuracy simulations of optical propagation in nanophotonic devices

We introduce a new high accuracy second-order finite-difference time-domain (FDTD) algorithm based on non-standard finite differences, and use it to investigate light propagation in subwavelength structures such as photonic crystals.     

Fluctuation of the Free Energy of Sherrington–Kirkpatrick Model with Curie–Weiss Interaction: The Paramagnetic Regime

Journal of Statistical Physics - We consider a spin system containing pure two spin Sherrington–Kirkpatrick Hamiltonian with Curie–Weiss interaction. The model where the spins are...     

Nonlocal time-delayed feedback control of spatiotemporal patterns: controlling a network of digital phase-locked loops

Nonlinear Dynamics - Control of spatially extended systems is an important and challenging topic of research. Previous control techniques rely on local or global feedback control. In this paper,...     

Preparation of 125I-Lanreotide and its biodistribution in murine model of melanoma

Lanreotide, a somatostatin analogue, was radioiodinated with ¹²⁵I to explore the possibility of using ¹²³I labeled lanreotide as a diagnostic radiopharmaceutical for tumors overexpressing somatostatin (SST) receptors. Radioiodination was carried out with ¹²⁵I using chloramine T as the oxidant. The labeling yield was >90%. Characterization of ¹²⁵I-Lanreotide was carried out by paper electrophoresis as well as HPLC. ¹²⁵I-Lanreotide was purified by chromatography using a C18 Sep-Pak column. Radiochemical purity of the purified ¹²⁵I-Lanreotide thus obtained was >99%. Significant tumor uptake of ¹²⁵I-Lanreotide was observed in C57BL/6 mice bearing melanoma.     

Production of Bioactive Compounds with Broad Spectrum Bactericidal Action,Bio-Film Inhibition and Antilarval Potential by the Secondary Metabolites of the Endophytic Fungus Cochliobolus sp. APS1 Isolated from the Indian Medicinal Herb Andrographis paniculata

Endophytes, being the co-evolution partners of green host plants, are factories of pharmaceutically valuable novel natural products. Cochliobolus sp. APS1, an endophyte of Andrographis paniculata (Green Chiretta), produces a plethora of natural bioactive compounds and the multipotent alkaloid Aziridine, 1-(2-aminoethyl)-, is the prime one among them. The isolate exhibited antibacterial, anti-biofilm, and antilarval potency. The MIC and MBC values of the ethyl-acetate culture extract ranged from 15.62 to 250 µg/mL against ten pathogenic microorganisms (including MRSA and VRSA). Killing kinetics data along with the leakage of macromolecules into the extracellular environment supports the cidal activity of the antibacterial principles. The broad spectrum antibacterial activity of Aziridine, 1-(2-aminoethyl)-, was optimized by a one-variable-at-a-time system coupled with response surface methodology, which led to a 45% enhancement of the antibacterial activity. The maximum response (22.81 ± 0.16 mm of zone of inhibition against MRSA) was marked in 250 mL Erlenmeyer flask containing 90 mL potato dextrose broth supplemented with (g%/L) glucose, 9.7; urea concentration, 0.74; with medium pH 6.48; after 8.76 days of incubation at 26 °C. APS1 strongly inhibited biofilm formation in the tested pathogenic microorganisms and acts as a larvicidal agent against the Dengue-vector Aedes aegypti. This is probably the first report of Aziridine, 1-(2-aminoethyl)-, from any endophytic source. Cochliobolus sp. APS1 possesses industrial importance for the production of bioactive alkaloids.