Asymmetric synthesis of 4'-alpha-alkylcarbovir derivatives

Asymmetric synthesis of 4'-alpha-alkylcarbovir derivatives 3 were achieved based on Sakai's asymmetric alkylation of beta-keto esters. The key carbocyclic intermediate 12 was synthesized from 6 via an eleven-step sequence. Coupling of 12 with 2-amino-6-chloropurine followed by desilylation and subsequent hydrolysis gave the target compounds 3 in moderate yields.     

Analysis of course errors on CVOR antennas (including effects ofmutual coupling between elements)

A VHF omnidirectional radio range (VOR) is a navigation aid radio beacon facility, which provides aircraft with azimuth information relative to the VOR station in question as the origin. In Japan, two types of VOR-the conventional type (referred to as a CVOR) and the Doppler type (referred to as a DVOR)-are currently in use. An element known as the Alford loop antenna (ALA), which changes the loading reactance, is used for the VOR because the horizontally polarized wave and nondirectivity in the horizontal plane are preferred. A VOR antenna consists of a carrier antenna and a sideband antenna-an aircraft receives separate signals from these two antennas and compares them to obtain azimuth information. The mutual coupling between the elements forming the carrier and the sideband antenna affects the directivity of the single elements, resulting in errors in azimuth information. With the mutual coupling between the antenna elements being taken into consideration, a quantitative calculation was made by using the moment method-the results of the calculation made it clear that a loading reactance value of -320 Ω is better to make not mutually coupled elements nondirectional while a loading reactance value of -600 Ω is optimum to minimize the azimuth error of a CVOR     

Lipopolysaccharide primes human alveolar macrophages for enhanced release of superoxide anion and leukotriene B4: self-limitations of the priming response with protein synthesis

Human alveolar macrophages (AM) can produce potent reactive oxygen intermediates (ROI) and arachidonic acid metabolites (eicosanoids), which have important roles in host defense and the pathogenesis of some diseases of the lung. Bacterial lipopolysaccharide (LPS) is believed to cause profound lung injury and can prime mouse peritoneal macrophages for the enhanced secretion of ROI and eicosanoids. Therefore, we investigated the effect of LPS pretreatment on the ability of AM to release superoxide anions (O2-) and leukotriene B4 (LTB4). LPS can prime AM for the enhanced secretion of O2- and LTB4, regardless of whether they are derived from nonsmokers or smokers. Moreover, judging from the time-response characteristics, this priming for LTB4 release could be inhibited in the later stages of pretreatment, when the O2(-)-releasing capacity was enhanced. The priming inhibition was prevented, at least in part, by cycloheximide, but not by SOD and/or catalase. In addition, cycloheximide also inhibited the priming for O2- release. Hence, protein synthesis might be necessary for the priming for O2- release and for inhibiting the priming for LTB4 release. This phenomenon of self-limiting the priming response with LPS seems to be very important when we consider the high oxygen tension in the lungs and the many bacterial substances inspired into alveoli.     

Polarization characteristics of poly(vinyl alcohol) films containing metal iodide

The polarization properties of iodine complex layer deposited by oxidation of poly(vinyl alcohol) (PVA) containing metal iodide were investigated. Heat-resistant polarizing films with high polarization efficiency were produced by oxidizing and stretching the PVA containing metal iodide. The results indicate that i) the polarization efficiency of a polarizing film prepared by oxidation of a PVA film containing 1 mmol or more of potassium iodide (KI)/g PVA at 0°C for 120 s in a 10 wt.-% aqueous solution of H₂O₂ and a degree of stretching of 400% is high, ii) the heat resistance of the polarizing film in this experiment is higher than that of a filter prepared from a commercial PVA film.     

YM-32890 A and B, new types of macrolide antibiotics produced by Cytophaga sp

Two new types of macrolide antibiotics, YM-32890 A and B, have been isolated from the fermentation broth of cytophaga sp. YL-02905S. In this paper, the taxonomy of the producing strain, fermentation, isolation, structure elucidation, and biological activity of the antibiotics are reported. YM-32890 A inhibits the growth of staphylococci including a macrolide-resistant strain, but shows no antimicrobial activity against other Gram-positive, Gram-negative bacteria and yeast.     

Influence of refraction on the visual field defects in normal tension glaucoma and primary open angle glaucoma eyes

The prevalence of normal tension glaucoma (NTG) or primary open angle glaucoma (POAG) is higher in myopic populations and the prevalence of myopia and NTG is relatively high in the Japanese. To evaluate the influence of myopic refractive error on the central visual field defect in NTG eyes, the data obtained from NTG eyes with the Humphrey Visual Field Analyser were analysed in comparison with those from POAG eyes. One hundred and twenty NTG eyes and one hundred and ninety-seven POAG eyes were included. All of them had clear ocular media, but no myopic degeneration in the fundus. Multiple linear regression analysis was performed with a dependent variable of the deviation of the measured threshold value from normal reference value (total deviation, STATPAC) and independent variables of refractive error and mean deviation (STATPAC). Myopic power was found to be positively correlated with the depression in the lower papillo-macular area in both NTG and POAG eyes, and it was negatively correlated with the depression in an upper arcuate area extending just nasal to the fixation only in NTG eyes.     

Attenuation of anticonvulsant effects of diazepam after chronic treatment with bicuculline

Changes in the GABAergic system after chronic treatment with bicuculline were examined in two strains of inbred rats, Fischer 344 (F344) and Lewis (LEW). Rats received an IP injection of either bicuculline (2 mg/kg) or vehicle once a day for 12 days. After this chronic treatment, the effects of diazepam (1 mg/kg, IP) and pentobarbital (20 mg/kg, IP) on bicuculline-induced convulsions were measured. Bicuculline was acutely infused into a tail vein at 0.0415 mg/min, and the infusion was terminated when rats showed seizure. Following the chronic bicuculline treatment, the anticonvulsant effect of diazepam, but not of pentobarbital, was significantly reduced as compared to its effect following chronic vehicle treatment in both strains. Both diazepam and pentobarbital showed a significant difference in anticonvulsant effects between strains (F344 > LEW). The hypnotic effects of muscimol, barbital, pentobarbital, and ethanol following chronic bicuculline treatment were examined. There was no significant difference in sleep time induced by these drugs between bicuculline- and vehicle-treated rats. These results suggest that the attenuation of diazepam's anticonvulsant effect after chronic bicuculline treatment may result from functional changes in benzodiazepine receptors and that the anticonvulsant effects of diazepam and pentobarbital may be influenced by genetic factors. Moreover, the hypnotic effects of several drugs tested are apparently not affected by chronic bicuculline treatment.     

A sensorless brushless dc motor system

This paper describes a brushless dc motor system without position or speed sensor. The brushless motor consists of a permanent magnet synchronous motor and a voltage-source inverter capable of controlling the amplitude and frequency of voltage. The rectangular-shaped stator current with a conducting interval of 120° (electrical) is controlled to be in phase with the trapezoidal back electromotive force. This results in producing maximum torque. Variable speed is achieved by adjusting the average motor voltage similarly to chopper control of dc motors. In this paper, two sensorless position detecting methods, i.e., an “indirect method” suited for the lower-speed range and a “direct method” suited for the higher-speed range are proposed. The combination of the two makes it possible to detect the rotor position over a wide-speed range. Furthermore, a speed-sen-sorless PLL control is proposed in applying the principle of the direct method. Experimental results obtained from a prototype brushless dc motor are shown to confirm the validity of the sensorless drive. The starting procedure of the motor also is discussed because it is impossible to detect the rotor position at a standstill.