(³H) Tobramycin was used as a probe to determine the relationship between the structure of aminoglycoside antibiotics and their ability to remove this drug from its higher affinity binding site on the ribosome. The dissacharide moieties (neamine, tobramine, gentamine) appeared to have a common binding site, whereas the kanosamine, garosamine and ribose moieties determined the specificity of this binding. Amikacin and butikacin behaved in an anomalous manner in spite of their close structural relationship to tobramycin.

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The activities of tobramycin derivatives acetylated and ethylated on the '-N, 2'-N and 3-N positions were examined. The MICs of these derivatives against tobramycin sensitive strains indicated that 2'-N-ethylated and '-N-ethylated derivatives have a fairly good activity, and confirmed that the 3-N position is the most important one for antibiotic activity since 3-N derivatives were less active. The MICs of these derivatives against tobramycin resistant strains, and their inactivation by tobramycin modifying enzymes were examined. These results showed that 2'-N or '-N ethylation protects the drug against inactivation by AAC(2') or AAC('), respectively, and 2'-N-ethyltobramycin and '-N-ethyltobramycin were active against strains containing these modifying enzymes. On the other hand, 3-N ethylation protects the drug against inactivation by AAC(3) but 3-N-ethyl tobramycin does not inhibit strains containing this enzyme.

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Repetitive liquefactions in angular and subangular gravels from an alluvial fan, in the case of two earthquakes with accelerations lower than that of a former which had caused liquefaction some months before, are described. The liquefaction took place from the surface, down to a depth of approximately 10 m. Water laden with sediments spouted out for some tens of minutes after the strong motion ceased. Knowledge of the grain size distribution of the sediments inside the body of the alluvial fan roughly defines the areas of the fan prone to future liquefaction. Non-repetitive liquefaction in overconsolidated fine fluvio-lacustrine sand of glacial origin at the unusual depth of 14 m to 16 m is also described. From the observation of sand lifted up for 10 m inside a large diameter well, and of that which spouted out from several microvents, it was estimated that extra-pore pressure was close to lithostatic conditions. Nevertheless, modeling of intrinsic pore pressure buildup on the DESRA2 programme gives lower values than the experimental one. Geotechnical characteristics of the 12 m-thick sandy stratum indicate that the upper part is unusually soft, either due to water circulation or past repetitive liquefactions which prevented reconsolidation. It is suggested that excess pore pressure generated by the earthquake was also due to redistribution of pressure from adjacent sediments.

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Leakage of water due to internal erosion through a dam body or foundation is a major problem with fill-type dams. Recent case histories and research suggest that most cases of internal erosion are possibly triggered by hydraulic fracturing. However, the quantitative mechanism of hydraulic fracturing still remains to be solved. Therefore in-situ hydraulic fracture tests were carried out with a cheap, concise apparatus using boreholes dug in the soft clayey volcanic soil foundation of a low earth dam (Oyachi Dam) in Niigata Prefecture. Water was injected into the foundation through a perforated pipe by two methods : one was under a controlled injection pressure and the other was a controlled injection flow rate. In the former method, the relationship between flow rate and injection pressure was observed and it was found that a yield pressure or fracture pressure existed in all the tests. By repeating the injection test it was confirmed that once a crack is developed, it is very easily reopened by a water pressure a little higher than the earth pressure exerted on the crack. In the latter method, the relationship between injection pressure and time was observed and it was found that fracture pressure varied with flow rate. The boreholes were excavated to observe the development of fracture cracks and it was also found that the cracks had developed perpendicular to the borehole periphery, which means that fracture cracks were induced by tensile stress and denies the explanation that fractures are caused by shear failure.

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A sample of [³H] tobrarnycin (, 000 Ci/Mole) has been synthetized and incubated with
the bacterial ribosome and its subunits. The results obtained show that this antibiotic has
two types of binding sites. The primary one is probably responsible for the inhibition of
protein synthesis whereas the secondary one is probably related to the misreading and reading
tiirough of the messenger RNA.

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The Beckmann rearrangement of aliphatic ketone oximes, R(CHs)=NOH (R=Et (1); n-Pr (2); iso-Pr (3); iso-Bu (4)), with polyphosphoric acid (PPA), polyphosphate ester (PPE), and ester of phosphoric acid (2 P- R) was carried out and migratory ratios ((a)/(b) in eq. (1)) were determined, The results are shown in Fig.1, 2, and 3, respectively.
In Fig.1 and 2, the migratory ratios decrease with reaction time and nearly approach to the ratios of anti-alkyl form/syn-alkylform in benzene(A1) or DMSO(A2)except for (3) (See Table 1). From this fact, it has been found that PPA and PPE are inactive for isomerization of the oximes andanti-alkyl oximes rearrange faster than syn-alkyl ones. ln the case of (3), migratery ratios are smaller than Ai or A2. As acetonitrile is detected by GLC, it is presumed that fission has been occurred simultaneously with rearrangement in anti-alkyl oxime (eq. (3)). In the case of 2 P- R, all modes of the reaction arethe same as in above, except that the rate of fission is tnuch faster than that in PPA and PPE.
The reaction of anti-alkyl ketone oximes having a bulky grouphas been greatly influenced by the use of sterically demanding catalysts such asPPA, PPE, and 2 P- R.

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A comparative study of the static and dynamic response of a slope is carried out, using the large deformation theory of the updated Lagrangian formulation and the conventional infinitesimal theory. In the static analysis, a strength reduction method proposed by one of the authors is used to evaluate the safety factor of the slope. It is found that by the large deformation theory, the safety factor is larger than that calculated by the infinitesimal theory, and this difference becomes large along with the reduction of elastic modulus. In the dynamic analysis, it is observed that the large deformation theory gives smaller sliding displacement and larger response acceleration than the infinitesimal approach. It is concluded that in many cases the large deformation approach gives more adequate solutions.

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Syntheses of 4, , , 7, , -hexahydro-4, -methano--methylthiazolo [4, -] azocine (III) and 4, , , 7, , -hexahydro-4, -methano--methylthiazolo [, 4-] azocine (IV) are described. Thiazolization of 2-azabicyclo [3. 3. 1] nonan--one (V) gave the 2-aminothiazole (VII), which was converted into III by deamination, hydrolysis of the benzoyl group and Esch-weiler-Clarke N-methylation. The 2-hydroxyl derivative (XIII) was also synthesized. On the other hand, compound (IV) was synthesized by cyclization of the olefinic urethane (XXI) with phenylselenenyl chloride, as a key step. Deselenation of XXII with triphenyltin hydride followed by LiAlH₄ reduction gave IV. The urethane (XXI) was prepared from the 2-aminothiazole (XVIIa), which was obtained by condensation of the bromodiketone (XVI) and thiourea.

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Circuit techniques to enhance the linearity of input-voltage-to-current (V/I) conversion and to increase the output impedance of a current source by compensating for the low intrinsic gain of a transistor were introduced to realize a high-frequency operational transconductance amplifier (OTA) for a low supply voltage using sub-100-nm CMOS processes. Applying these techniques, a MOS 7th-order Gm- linear-phase low-pass filter (LPF) was realized using a 65nm CMOS process. A simplified biquad LPF that can serve as a component of a 7th-order LPF was newly developed by replacing OTAs with resistors. As a result, the -3dB frequency bandwidth, group delay ripple, 3rd-order distortion, and 3rd-order input intercept point (IIP3) were 200MHz, 2.2%, ≤ -55dB with a 100MHz input, and +10.3dBm, respectively, all with a ±0.1Vp-p input signal at each input terminal in the pseudodifferential configuration. The LPF including an output buffer dissipated 60mW in the case of a 1.2V supply. Wide spurious-free dynamic range (SFDR) characteristics were confirmed up to high frequencies.

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Based on the concept "intermediate soil wedge" which is dependent on mobilized frictional resistance, a new theory has been developed for evaluating the seismic earth pressures against retaining walls under any condition between the active and passive states. For this theory, the seismic earth pressure is separated into four components according to their formation. New equations are proposed to determine the distribution, resultant and point of application for each component. An equivalent seismic coefficient is introduced to take into account non-uniform seismic acceleration distribution with depth. The equations place special emphasis on dependence of the seismic earth pressure on mode and level of wall movement. The equations can be reduced to the Mononobe-Okabe equation for the limiting conditions. Their applicability was confirmed by comparing the predictions with a number of previous model test results.

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During earthquakes, saturated loose sandy soils often liquefy, causing serious damage to buildings and underground structures. Various construction methods have been employed to stabilize these soils against liquefaction. The popular methods are those which increase their density. Vibration and impact methods are commonly employed, but these often pose a problem of noise and vibration in urban areas. Results of previous experiments have shown that Quick Lime Consolidated Briquettes (QCB), a soil stabilizer made of quicklime and cement placed to form cylinders, significantly increases resistance to liquefaction by utilizing the effects of water absorption, swelling, and hardening. In the present study, shaking table tests were performed to evaluate the earthquake resistance of soil treated with QCB. Results of these test showed that the response acceleration and excess pore water pressure in QCB-treated soils were scarcely affected by the excitation of 200 Gals. The soil settlement due to shaking was about one tenth of that for the untreated soil, proving the effectiveness of QCB during earthquakes.

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A finite element model capable of taking into account nonlinear hysteretic soil behavior is presented to study earthquake induced retaining wall movement. The model also accounts for increase in lateral stresses and settlement associated with grain slip caused by cyclic loads. The predictive capability of the proposed method is verified by comparing responses given by the model with those computed by another existing finite element model and also with responses recorded at the Cambridge centrifuge facility. The study reveals that the wall displacement can be substantially affected, among other factors, by the increase in lateral stresses due to grain slip and wall-soil friction. Care should be taken when selecting a constant value of wall-soil friction angle for the entire duration of excitation since structural changes can occur in the soil adjacent to the wall.

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New-type inducers of differentiation of human promyelocytic leukemia cells HL-60, i.

e

., 4- (, , 7, -tetrahydro-, , , -tetramethyl-2-naphthalenylcarbamoyl) benzoic acid (Am 80) and () -4- [3- (3, -di-tert-butylphenyl) -3-oxo-l-propenyl] benzoic acid (Ch 55), suppress -myc expression as all-trans-retinoic acid (RA) does. The decreased level of -myc expression was detected within -14 h after the start of treatment, and preceded morphological differentiation and functional differentiation measured in terms of nitroblue tetrazolium (NBT) reduction. Treatment of HL-60 cells with 0.1 μm Am 80, Ch 55 or RA for 96 h caused more than % suppression of -myc expression and around 10-fold increase in the percentage of NBT-positive cells.

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The (S)-enantiomer of the sex pheromone of the yellow scale (Aonidiella citrina), (S, )--isopropyl-3, -dimethyl-, -decadienyl acetate, was stereoselectively synthesized from (R)-(+)-citronellic acid.

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