Parallel synthesis and in vitro activity of novel anthranilic hydroxamate-based inhibitors of the prostaglandin H2 synthase peroxidase activity

Currently available non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin are directed at the cyclooxygenase (COX) site, but not the peroxidase (POX) activity of prostaglandin H2 synthase (PGHS). They are thus unable to inhibit the free-radical induced tissue injury associated with PGHS peroxidase activity, which can occur independently of the COX site. A lead compound, anthranilic hydroxamic acid (AHA) was found to have significant PGHS-POX inhibitory activity (IC50= 72 microM). To define the critical parameters for PGHS-POX inhibition, we investigated 29 AHA derivatives, synthesised from their acid precursors, using solid phase synthesis. In vitro analysis demonstrated a ten-fold improvement in inhibition with 3,5-diiodoanthranilic hydroxamic acid (IC50= 7 microM).     

Laser Doppler anemometry

A brief survey is given of the principles and present state of the art in laser Doppler anemometry. Both the optical and signal-processing aspects are treated in some detail. The comparative features and special problems associated with the various methods of interpreting the Doppler signals are discussed, with particular reference to the more recently developed technique of photon correlation. A wide range of practical applications, including measurements on liquids and solids, is considered.     

Correlation functions of odd numbers of spins with finite separations on the Onsager-Ising lattice

A method is developed for making exact evaluations of correlation functions of odd numbers of spins on the Onsager-Ising lattice, applicable to cases in which the separations between the spins are finite. The method is based on an identity which permits the reduction of determinants of infinite-dimensional matrices to those of finite dimension. Particularly simple results are obtained when all spins are on a straight line. Numerical calculations are carried out for a few cases.     

怀孕期头发中一些元素含量的变化趋势

用同步辐射激发X射线荧光分析,对11个产妇怀孕期间头发内一些元素含量的变化趋势进行了测量,在各自对比的基础上,得到了一些结果。     

Tribocharging studies on inhabited cleanroom garments

Studies are reported on the surface voltages created on inhabited cleanroom garments when these are subject to tribocharging actions. It is shown that the voltage created per unit of charge does not depend on whether the garment fabrics include core conductive threads, giving very high surface resistivity values, or surface conductive threads, which show resistivity values well within the requirements of formal electrostatic Standards. Lower surface voltages per unit of charge are observed for the closer spacing of the conductive threads. These results call into question whether measurement of resistivity is the most appropriate basis for assessing the suitability of materials.     

Synthesis of orthogonally protected lanthionines

Synthetic approaches to the lantibiotics, a family of thioether-bridged antimicrobial peptides, require flexible synthetic routes to a variety of orthogonally protected derivatives of lanthionine 1. The most direct approaches to lanthionine involve the reaction of cysteine with an alanyl beta-cation equivalent. Several possibilities exist for the alanyl beta-cation equivalent, including direct activation of serine under Mitsunobu conditions: however, the low reactivity of sulfur nucleophiles in the Mitsunobu reaction has previously precluded its use in the synthesis of the lantibiotics. We report here a new approach to the synthesis of protected lanthionine, using a novel variant of the Mitsunobu reaction in which catalytic zinc tartrate is used to enhance the nucleophilicity of the thiol. In the course of these studies, we have also demonstrated that the synthesis of lanthionine from trityl-protected beta-iodoalanines is prone to rearrangement, via an aziridine, to give predominantly trityl-protected alpha-iodo-beta-alanines, and hence norlanthionines, as the major products.     

Analysis of long corona charge decay times

Studies on materials with long charge decay times (notably pharmaceutical powders) have shown that the local charge decay time constant comes to increase linearly with time during the progress of charge decay. This is an empirical result. This linear increase provides the basis for calculating the time to 1/e and/or to 10% from much shorter periods of observation than the times to achieve these decays. The approach involves simple numerical processing of the rate of increase in the local charge decay time constant with time and the intercept of this at some selected time. This analysis is useful for assessing and comparing materials that have decay times over say 10⁴ s.