An efficient method for the N-arylation of phenylurea via copper catalyzed amidation

The coupling reaction of phenylurea with different functionalized aryl halides in the presence of air stable CuI,N,N-dimethylethylenediamine as a ligand,and K₃PO₄ as a base gives symmetrical and unsymmetrical diarylureas in relatively high yields.This method is milder than the palladium catalyzed arylation and avoids the use of toxic phosphine ligands.     

Numerical study of exact Purcell factors in finite-size planar photonic crystal waveguides

The waveguide-length sensitivity on modified spontaneous emission in finite-size planar photonic crystal (PC) waveguides is investigated by numerically computing the exact Purcell (enhanced emission) factor. An unusual dependence on the number of waveguide unit cells and on the waveguide facet truncation is found, allowing one to nanoengineer large Purcell factors in excess of several hundred. Besides having important applications for single-photon sources, these results offer physical insight into the nature of light-matter interactions in miniaturized finite-size PC waveguides, where periodic Bloch-wave analysis breaks down.     

Computational design of novel cyclic urea as HIV-1 protease inhibitor

A series of novel cyclic urea molecules 5,6-dihydroxy-1,3-diazepane-2,4,7-trione as HIV-1 protease inhibitors were designed using computational techniques. The designed molecules were compared with the known cyclic urea molecules by performing docking studies, calculating their ADME (Absorption, Distribution, Metabolism, and Excretion) properties and protein ligand interaction energy. These novel molecules were designed by substituting the P ₁/P′ ₁ positions (4 ^th and 7 ^th position of 1, 3-diazepan-2-one) with double bonded oxygens. This reduces the molecular weight and increases the bioavailability, indicating better ADME properties. The docking studies showed good binding affinity towards HIV-1 protease. The biological activity of these inhibitors were predicted by a model equation generated by the regression analysis between biological activity (log 1/K ⁱ ) of known inhibitors and their protein ligand interaction energy. The synthetic studies are in progress.      

Metal-sensitive and thermostable trypsin from the crevalle jack (<Emphasis Type="Italic">Caranx hippos</Emphasis>) pyloric caeca: purification and characterization

Background

Over the past decades, the economic development and world population growth has led to increased for food demand. Increasing the fish production is considered one of the alternatives to meet the increased food demand, but the processing of fish leads to by-products such as skin, bones and viscera, a source of environmental contamination. Fish viscera have been reported as an important source of digestive proteases with interesting characteristics for biotechnological processes. Thus, the aim of this study was to purify and to characterize a trypsin from the processing by-products of crevalle jack (Caranx hippos) fish.

Results

A 27.5 kDa trypsin with N-terminal amino acid sequence IVGGFECTPHVFAYQ was easily purified from the pyloric caeca of the crevalle jack. Its physicochemical and kinetic properties were evaluated using N-α-benzoyl-_DL-arginine-p-nitroanilide (BApNA) as substrate. In addition, the effects of various metal ions and specific protease inhibitors on trypsin activity were determined. Optimum pH and temperature were 8.0 and 50°C, respectively. After incubation at 50°C for 30 min the enzyme lost only 20% of its activity. K _m , k_cat, and k _cat /K _m values using BApNA as substrate were 0.689 mM, 6.9 s^-1, and 10 s^-1 mM^-1, respectively. High inhibition of trypsin activity was observed after incubation with Cd²⁺, Al³⁺, Zn²⁺, Cu²⁺, Pb²⁺, and Hg²⁺ at 1 mM, revealing high sensitivity of the enzyme to metal ions.

Conclusions

Extraction of a thermostable trypsin from by-products of the fishery industry confirms the potential of these materials as an alternative source of these biomolecules. Furthermore, the results suggest that this trypsin-like enzyme presents interesting biotechnological properties for industrial applications.

     

Fission products from the damaged Fukushima reactor observed in Hungary

Fission products, especially ¹³¹I, ¹³⁴Cs and ¹³⁷Cs, from the damaged Fukushima Dai-ichi nuclear power plant (NPP) were detected in many places worldwide shortly after the accident caused by natural disaster. To observe the spatial and temporal variation of these isotopes in Hungary, aerosol samples were collected at five locations from late March to early May 2011: Institute of Nuclear Research, Hungarian Academy of Sciences (ATOMKI, Debrecen, East Hungary), Paks NPP (Paks, South-Central Hungary) as well as at the vicinity of Aggtelek (Northeast Hungary), Tapolca (West Hungary) and Bátaapáti (Southwest Hungary) settlements. In addition to the aerosol samples, dry/wet fallout samples were collected at ATOMKI, and airborne elemental iodine and organic iodide samples were collected at Paks NPP. The peak in the activity concentration of airborne ¹³¹I was observed around 30 March (1–3 mBq m^?3 both in aerosol samples and gaseous iodine traps) with a slow decline afterwards. Aerosol samples of several hundred cubic metres of air showed ¹³⁴Cs and ¹³⁷Cs in detectable amounts along with ¹³¹I. The decay-corrected inventory of ¹³¹I fallout at ATOMKI was 2.1±0.1 Bq m^?2 at maximum in the observation period. Dose-rate contribution calculations show that the radiological impact of this event at Hungarian locations was of no considerable concern.