Total Synthesis and Biological Evaluation of the Antibiotic Lysocin E and Its Enantiomeric,Epimeric, and N‐Demethylated Analogues

Lysocin E, a macrocyclic peptide, exhibits potent antibacterial activity against methicillin‐resistant Staphylococcus aureus (MRSA) through a novel mechanism. The first total synthesis of lysocin E was achieved by applying a full solid‐phase strategy. The developed approach also provides rapid access to the enantiomeric, epimeric, and N‐demethylated analogues of lysocin E. Significantly, the antibacterial activity of the unnatural enantiomer was comparable to that of the natural isomer, suggesting the absence of chiral recognition in its mode of action.     

Hydrogen bonding effects on the wavenumbers and absorption intensities of the OH fundamental and the first, second, and third overtones of phenol and 2,6-dihalogenated phenols studied by visible/near-infrared/infrared spectroscopy

Visible, near-infrared (NIR) and IR spectra in the 15600-2500 cm(-1) region were measured for phenol and 2,6-difluorophenol, 2,6-dichlorophenol, and 2,6-dibromophenol in n-hexane, CCl(4), CHCl(3) and CH(2)Cl(2) to study hydrogen bonding effects and solvent dependences of wavenumbers and absorption intensities of the fundamental and the first, second, and third overtones of OH stretching vibrations. A band shift of the OH stretching vibrations from a gas state to a solution state (solvent shift) was plotted versus vibrational quantum number (v = 0, 1, 2 and 3), and it was found that there is a linear relation between the solvent shift and the vibrational quantum number. The slope of solvent shift decreases in the order of phenol, 2,6-difluorophenol and 2,6-dichlorophenol. For all of the solute molecules, the slope becomes larger with the increase in the dielectric constant of the solvents. The relative intensities of the OH stretching vibrations of phenol in CCl(4), CHCl(3), and CH(2)Cl(2) against the intensity of the corresponding OH vibration in n-hexane increase in the fundamental and the second overtone but decrease in the first and third overtones; the relative intensities show so-called "parity". The parity is more prominent for phenol that has an intermolecular hydrogen bonding than for 2,6-dihalogenated phenols that have an intramolecular hydrogen bond. These observations suggest that the intermolecular hydrogen bond between the OH group and the Cl atom plays a key role for the parity and that the intermolecular interaction between the solutes and the solvents (solvent effects) does not have a significant role in the parity.     

Core-polarization effects on the magnetic transitions in the 208Pb region

We show that there is a reduction of the magnetic transition strength at high momentum transfer due to core polarization. This accounts substantially for the observed reduction of 50% of the J^π=12^? and 14^? transitions in ²⁰⁸Pb. The core polarization does not affect the shape of the high J form factors in the vicinity of their main peaks. However, a significant q-dependent effect is predicted for the ground state M1 moment of ²⁰⁷Pb.     

Electrochemical reactors for NO decomposition. Basic aspects and a future

The electrochemical reduction of nitric oxide in the presence of the excess oxygen was reviewed. It was shown that the selectivity and activity of the cathodes is strongly dependent on the composition and on the microstructure of the cathode material. A concept of electrochemical reactor with multilayer electro-catalytic electrode was proposed and successfully designed in Advanced Manufacturing Research Institute, National Institute of Advanced Industrial Science and Technology (AIST), Nagoya, Japan. The typical values of current efficiency in such electrochemical reactors are of the order of 10–20% at gas composition: 1,000 ppm NO and 2% O₂ balanced in He and at gas flow rate 50 ml/min. The value of current efficiency depends on the functional multi-layer electrode composition, structure, and operating temperature. Such electrochemical reactors show the value of NO/O₂ selectivity (ν _sel) higher than 5 (ν _sel > 5) at intermediate temperature and up to ν _sel = 25 at low temperature operation. It was shown that multilayer electro-catalytic electrode should consist at list from three main functional layers: cathode, electro-catalytic electrode, covering layer, in order to operate as an electrode with high selectivity.     

Index-of-refraction sensors: virtually unlimited sensing power at the critical angle

In an effort to improve and simplify refractive index sensors, we identified a basic operation mode at the critical angle. Sensitivity to the refractive index is higher than in standard surface plasmon resonance sensors, and we have been able to demonstrate analytically that it is virtually an unbounded value. We describe this approach and submit a complete analytical study demonstrating its unlimited sensing power. To test the approach, we constructed an economical and basic sensor. Despite its simplicity, we demonstrated the discrimination capability to be of the order of 10(-6), as far as we know close to the best sensitivity ever recorded. This detection method is generally applicable to any optical system and may pave the way for the next generation of optical sensing devices.     

Species Differences in Metabolism of Soluble Epoxide Hydrolase Inhibitor,EC1728, Highlight the Importance of Clinically Relevant Screening Mechanisms in Drug Development

There are few novel therapeutic options available for companion animals, and medications rely heavily on repurposed drugs developed for other species. Considering the diversity of species and breeds in companion animal medicine, comprehensive PK exposures in the companion animal patient is often lacking. The purpose of this paper was to assess the pharmacokinetics after oral and intravenous dosing in domesticated animal species (dogs, cats, and horses) of a novel soluble epoxide hydrolase inhibitor, EC1728, being developed for the treatment of pain in animals. Results: Intravenous and oral administration revealed that bioavailability was similar for dogs, and horses (42 and 50% F) but lower in mice and cats (34 and 8%, respectively). Additionally, clearance was similar between cats and mice, but >2× faster in cats vs. dogs and horses. Efficacy with EC1728 has been demonstrated in mice, dogs, and horses, and despite the rapid clearance of EC1728 in cats, analgesic efficacy was demonstrated in an acute pain model after intravenous but not oral dosing. Conclusion: These results demonstrate that exposures across species can vary, and investigation of therapeutic exposures in target species is needed to provide adequate care that addresses efficacy and avoids toxicity.     

Multilayered electrochemical cell for NOx decomposition at moderate temperatures

A new multilayered electrochemical cell for NO_x decomposition was prepared. The cell demonstrated good characteristics at moderate temperatures (350–450 °C) and possessed much higher selectivity with respect to NO_x decomposition than previous one. It was found that the “crossover” process from high selective regime to the normal regime depends on the chemical composition of the catalytic electrode.     

A novel and useful oxidative intramolecular coupling reaction of phenol ether derivatives on treatment with a combination of hypervalent iodine(III) reagent and heteropoly acid

The oxidative intramolecular coupling reaction of phenol ether derivatives (nonphenolic derivatives) on treatment with a novel combination of a hypervalent iodine(III) reagent, phenyliodine bis(trifluoroacetate) (PIFA), and heteropoly acid (HPA) was studied. Biaryl compounds were obtained in excellent yields on treatment of highly substituted phenol ethers. On the other hand, spirodienones were specifically formed when one of the preferred arylic coupling sites was substituted with a methoxy group in the para position.     

An expansion of system with time delayed feedback control into spatio-temporal state space

Time delayed feedback control is well known as an effective continuous control method for stabilizing the unstable periodic orbit embedded in chaotic attractors. As for the system with time delay, the solution is in a function space and shows characteristics governed by an infinite dimension. Therefore it is difficult to understand the system behavior analytically. In this paper, it is shown that, when the state space for the system with time delay is expanded into the spatio-temporal state space, the solution propagates in the space as a wave theoretically and numerically. The dynamic behavior experimentally obtained in the sinusoidally excited magneto-elastic beam system under time delayed feedback control is also discussed by the transformation into the expanded spatio-temporal state space. (c) 1999 American Institute of Physics.