Ugi three-component reaction of alcohols,amines and isocyanides: A new approach to the synthesis of cyclic amidines

We have developed a novel, simple, efficient and one pot synthetic protocol for the synthesis of cyclic amidines via Ugi three-component reaction of alcohols, amines, and isocyanides.     

Reverse elution order of β-blockers in chiral separation

In the field of chiral separation, the elution order of the enantiomers is one of the most important phenomena. Although the reversal of enantiomeric elution order is rare, it has certain significance. In the determination of the optical purities, the study of this phenomenon is helpful because it is favorable to elute the minor enantiomeric impurity before the major component. This mini review reports the reversal order of elution of the most important class of the drugs of β-blockers. This mini review describes the effects of the composition of the mobile phase, pH, and temperature on the reversal order of elution of β-blockers. The efforts are also made to discuss the possible future perspectives of reversal order of elution.     

Free radical scavenging phenylethanoid glycosides from Leucas indica Linn

A new phenylethanoid glycoside, 2-(3,4-dihydroxyphenyl)-ethyl-O-alpha-L-rhamnopyranosyl-(1 --> 3)-O-alpha-L-rhamnopyranosyl-(1 --> 6)-4-O-E-feruloyl-beta-D-glucopyranoside (3-O-methyl poliu-moside, 1) along with five known phenylethanoid glycosides (2-6) were isolated from the aerial parts of Leucas indica Linn. The structure of compound 1 has been elucidated on the basis of spectral data. Compounds 1-6 exhibited significant antioxidant activity in 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical assay method. These compounds were also found to be moderate inhibitors of xanthine oxidase (XO) enzyme.     

N-Methyl substituted 2',4'- BNANC: a highly nuclease-resistant nucleic acid analogue with high-affinity RNA selective hybridization

Oligonucleotides modified with a novel BNA analogue, 2', 4'-BNA(NC)[N-Me], were synthesized, and in comparison to 2',4'-BNA (LNA), have similarly high RNA affinity, better RNA selectivity and much higher resistance to nuclease degradation, suggesting that the novel BNA analogue may be particularly useful for antisense approaches.     

High precision quantum control of single donor spins in silicon

The Stark shift of the hyperfine coupling constant is investigated for a P donor in Si far below the ionization regime in the presence of interfaces using tight-binding and band minima basis approaches and compared to the recent precision measurements. In contrast with previous effective mass-based results, the quadratic Stark coefficient obtained from both theories agrees closely with the experiments. It is also shown that there is a significant linear Stark effect for an impurity near the interface, whereas, far from the interface, the quadratic Stark effect dominates. This work represents the most sensitive and precise comparison between theory and experiment for single donor spin control. Such precise control of single donor spin states is required particularly in quantum computing applications of single donor electronics, which forms the driving motivation of this work.     

Sensitive and selective determination of peptides,PG and PGP,using a novel fluorogenic reagent 4-chlorobenzene-1,2-diol

A novel fluorometric method was developed for the sensitive and selective detection of Pro-Gly (PG) and Pro-Gly-Pro (PGP) using 4-chlorobenzene-1,2-diol (4-CBD) as a fluorogenic reagent. The reaction was performed at 37°C for 30 min in the presence of a borate buffer (pH 7.0) and sodium periodate. The resulting fluorescence intensity was measured using a spectrofluorometer with excitation and emission wavelengths of 450 nm and 535 nm. To obtain a stable fluorescent signal and maximise its intensity, different reaction conditions such as the concentrations of the reagents, the reaction time, and the pH were optimised. Under the optimised conditions, a linear relationship was obtained between fluorescence intensity and peptide concentrations from 1.0–40.0 µmol L^?1 with a limit of detection of 1.0 µmol L^?1 (S/N = 3). Both PG and PGP generated a strong signal out of all the peptides tested and no other biogenic substances such as amino acids or proteins produced any fluorescence. The reaction thus developed is simple, rapid, selective, and sensitive. It can be applied to the determination of peptides as biomarkers or substrates.     

Use of quadrupole time of flight mass spectrometry for the characterization of transformation products of the antibiotic sulfamethazine upon photocatalysis with Pd‐doped ceria‐ZnO nanocomposite

The photocatalytic degradation of the antibiotic sulfamethazine under excitation at 365 nm of Pd‐doped ceria‐ZnO nanocomposite, titanium dioxide and iron(III) aqua complex was deeply studied from the analytical point of view. It reveals the formation of nine degradation products that were detected in their protonated forms using LC/electrospray ionization quadrupole time‐of‐flight MS in the positive mode. Their formation involves the hydroxyl radical, and their concentrations increased with irradiation time. Collision‐induced dissociation tandem mass spectrometry associated with the accurate mass measurements was efficiently used for the elucidation of their chemical structures. None of these identified degradation products has been already reported in the literature. Three by‐products result from the hydroxylation at the pyrimidine moiety as well as at the aromatic part, two of them arise from the scission of the pyrimidine group, and finally, three of them come from the scission of the sulfamide bridge. This points the evidence of studying the fate of these degradation products if their toxicity is demonstrated because they are clearly the result of the reaction of hydroxyl radical with the antibiotic sulfamethazine. Copyright © 2015 John Wiley & Sons, Ltd.