Improved methods for thermal rearrangement of alicyclic α-hydroxyimines to α-aminoketones: synthesis of ketamine analogues as antisepsis candidates

Ketamine is an analgesic/anesthetic drug, which, in combination with other drugs, has been used as anesthetic for over 40 years. Ketamine induces its analgesic activities by blocking the N-methyl-D-aspartate (NMDA) receptor in the central nervous system (CNS). We have reported that low doses of ketamine administrated to patients before incision significantly reduced post-operative inflammation as reflected by reduced interleukin-6 (IL-6) sera-levels. Our data demonstrated in a rat model of Gram-negative bacterial-sepsis that if we inject a low dose of ketamine following bacterial inoculation we reduce mortality from approximately 75% to 25%. Similar to what we have observed in operated patients, the levels of TNF-α and IL-6 in ketamine-treated rats were significantly lower than in septic animals not treated with ketamine. On the base of these results, we have designed and synthesized series of new analogues of ketamine applying a thermal rearrangement of alicyclic α-hydroxyimines to a-aminoketones in parallel arrays. One of the analogues (compound 6e) displayed high activity in down-regulating the levels of IL-6 and TNF-α in vivo as compared to ketamine.     

Scaling, Optimality, and Landscape Evolution

A nonlinear model is studied which describes the evolution of a landscape under the effects of erosion and regeneration by geologic uplift by mean of a simple differential equation. The equation, already in wide use among geomorphologists and in that context obtained phenomenologically, is here derived by reparametrization invariance arguments and exactly solved in dimension d=1. Results of numerical simulations in d=2 show that the model is able to reproduce the critical scaling characterizing landscapes associated with natural river basins. We show that configurations minimizing the rate of energy dissipation (optimal channel networks) are stationary solutions of the equation describing the landscape evolution. Numerical simulations show that a careful annealing of the equation in the presence of additive noise leads to configurations very close to the global minimum of the dissipated energy, characterized by mean field exponents. We further show that if one considers generalized river network configurations in which splitting of the flow (i.e., braiding) and loops are allowed, the minimization of the dissipated energy results in spanning loopless configurations, under the constraints imposed by the continuity equations. This is stated in the form of a general theorem applicable to generic networks, suggesting that other branching structures occurring in nature may possibly arise as optimal structures minimizing a cost function.     

Fusion around the barrier for 7Li+12C

Fusion cross-sections for the ⁷Li + ¹²C reaction have been measured at energies above the Coulomb barrier by the direct detection of evaporation residues. The heavy evaporation residues with energies below 3 MeV could not be separated out from the α-particles in the spectrum and hence their contribution was estimated using statistical model calculations. The present work indicates that suppression of fusion cross-sections due to the breakup of ⁷Li may not be significant for ⁷Li + ¹²C reaction at energies around the barrier.     

Axial heat conduction effects in the entrance region of circular ducts

This paper describes the transport of thermal energy within a small distance after an abrupt wall temperature change in a circular duct. In general, the axial conduction becomes significant when the Peclet number is small. The results indicate that the inclusion of axial conduction in the fluid substantially increases the wall heat flux at near the thermal inlet location. The exact series solution leads to a modified Graetz type problem. This exact solution is augmented by an asymptotic solution describing the wall heat flux near the thermal entrance location.     

Antimicrobial active packaging combining essential oils mixture: Migration and odor control study

Thymol is an essential oil (EO), known to have excellent antimicrobial (AM) properties and can potentially be used as an active agent in AM food packages. Mixing Thymol with other EOs may help to reduce the organoleptic impact of its strong odor. In the present study, the effect of thymol, carvacrol, citral, and eugenol binary mixtures on the AM activity, migration over time, and sensory properties of polypropylene (PP)/polyamide (PA)/nanoclays composite blends active package (AP) films was examined. The release of different EOs from the polymer film was found to have a direct correlation with the odor perception of thymol. Varied EOs bearing films have shown different capacity to inhibit bacterial growth over time (Escherichia coli). Lastly, the inhibition of fungal growth on food sample using EO‐loaded films was obtained for over 50 days, indicating the potential use of the developed films as active food packaging.     

Radiation from a Charge Supported in a Gravitational Field

We examine whether a charge supported statically in a gravitational field radiates, and find the answer to this question to be positive. Based on our earlier results we find that the important condition for the creation of radiation is the existence of a relative acceleration between the charge and its electric field, where such an acceleration causes the curving of the electric field and the creation of a stress force due to this curvature. This stress force is the reaction force, which creates the radiation. Later we find that this condition do exist for a charge supported statically in a gravitational field, where the electric field of the charge falls in the gravitational field, it curves, and the stress force raised in this curved field, creates electromagnetic radiation.     

Crystal and molecular structure of hydroxyjatrophone C

The structure of the title compound has been established by means of the x-ray diffraction method on a single crystal. The crystals are othorhombic, space groupP2₁2₁2₁ (No. 19) witha=10.222(4),b=10.622(2),c=16.434(3) Å,z=4. Full-matrix least squares refinement led toR=4.9%. The molecular stereochemistry, bond distances, bond angles, torsion angles, and hydrogen bond scheme have all been determined.Camille and Henry Dreyfus Teacher Scholar, 1978–1983; National Institutes of Health (National Cancer Institute) Career Development Award, 1980–1985.     

A Time of Flight Model for Cloud’s Radiative Transfer

A model for fast calculation of path radiance of finite clouds is presented. The calculations are simplified by using the reciprocity principle and the homogenousness property of the incident light. Comparisons with reasonably accurate calculations for spherical cloud and two-dimensional infinite layer were made.Presented at the 7th International Workshop on Multiple Scattering Lidar/Light Experiments (MUSCLE7), July 21–23 1994, Chiba, Japan.     

A short story of SIN!

A brief overview is given of the theory of surface-ion neutralization (SIN) by highlighting studies from the pioneering days to the present time. Emphasis is placed on the 1-electron time-dependent Newns-Anderson (TDNA) model, which has played such a key role in studying resonance charge transfer. Recently, a many-electron (ME) version of the TDNA approach has been formulated to treat two or more electron processes, such as Auger transitions. The equation-of-motion technique is used to obtain the TD coefficients from which the required SIN probabilities can be found. After outlining the ME method, two applications are described. The first deals with the Li⁺-Cs/W(110) system, while the second addresses the laser enhancement of SIN, in the case of Li⁺-KBr, and revises some earlier results.     

STOCHASTIC ENERGY DEMAND AND THE STABILIZATION VALUE OF ENERGY STORAGE

The economic value of energy storage to meet peak electricity demand is analyzed with an emphasis on the role of demand uncertainty. The concept of the stabilization value, which measures that part of the benefit of the storage project which is due solely to the stochastic demand components, is defined. The magnitude of the stabilization value, relative to the overall value of energy storage, is evaluated in terms of a simple model that accounts for the relevant characteristics of the electric power utility's production mix. It is found that neglecting the demand uncertainty can seriously bias the benefit assessment of the storage project as well as the determination of the optimal storage capacity.