A sample of [

3H

] tobrarnycin (

5

, 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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(

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 -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 -N position is the most important one for antibiotic activity since -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, -N ethylation protects the drug against inactivation by AAC() but -N-ethyl tobramycin does not inhibit strains containing this enzyme.

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Two new partially saturated tricyclic ring systems, , a, , , , 10, 10a, 11-octahydro-11-oxodibenz [, ] oxepins (a and ), and -thiepins (a and ) were synthesized. Compounds a and were desulfurized to give a pair of isomeric 2-methylbenzoylcyclohexanes (10a and 10). Deuterated a and (11a and 11) were prepared starting from butadiene- (12). The stereochemical features of a (trans), (cis), a (trans) and (cis) are compared with those of 10a, 10, 11a and 11 on the basis of proton nuclear magnetic resonance data.

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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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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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11-Amino-, a, , , , 10, 10a, 11-octahydrodibebenzo[, ]thiepines (a-d) and -oxepines (a-d) were synthesized by the Leuckart reaction of , a, , , , 10, 10a, 11-octahydro-11-oxodibenzo[, ]thiepines (a, )and -oxepines (2a, ) followed by hydrolysis of the reaction products a-d and a-d, respectively. The four diastereomers, cis(a-H, 10a-H)-cis(10a-H, 11-H) a and a, cis(a-H, 10a-H)-trans(10a-H, 11-H) and , trans(a-H, 10a-H)-trans(10a-H, 11a-H) and , and trans(a-H, 10a-H)-cis(10a-H, 11-H) d and d, were isolated and their configurations and conformations were elucidated by chemical methods together with

1H

-nuclear magnetic resonance spectroscopic and X-ray crystallographic analyses.

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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 th-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 th-order LPF was newly developed by replacing OTAs with resistors. As a result, the -dB frequency bandwidth, group delay ripple, rd-order distortion, and rd-order input intercept point (IIP) were 200MHz, 2.2%, ≤ -55dB with a 100MHz input, and +10.dBm, respectively, all with a ±0.Vp-p input signal at each input terminal in the pseudodifferential configuration. The LPF including an output buffer dissipated 60mW in the case of a .2V supply. Wide spurious-free dynamic range (SFDR) characteristics were confirmed up to high frequencies.

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The ability of Climacodon septentrionalis to immobilize and kill a mycophagous nematode (Aphelenchoides sp.) in vitro is described for the first time. Two isolates produced droplets (20–45 μm in diameter) that formed at the apices of tall, stalked, and branching secretory cells (700–

,500 μm tall). On 2% modified malt extract agar, nematodes became enveloped in the droplets, which restricted their ability to move and resulted in complete immobilization and death within several hours of contact. The rate of decomposition of the nematodes varied considerably, with most individuals persisting for weeks whereas others were degraded within several days and appeared to be colonized by dense hyphal growth. This study provides the first documentation of a non-agaricoid fungus producing secretory cells that are able to immobilize nematodes.

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Two new polyacetylene compounds (, , 12)--acetoxy--isovaleryloxytetradeca-, , 12-trien-, 10-diyn-14-ol (), and (, , 12)--acetoxy--(2-methylbutyryloxy)tetradeca-, , 12-trien-, 10-diyn-14-ol () have been isolated along with (, , 12)--acetoxy--senecioyloxytetradeca-, , 12-trien-, 10-diyn-14-ol (A) from Atractylodes Rhizome (Karabyakujutu). The structures of these compounds were determined on the basis of their spectral data.

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The correction factor (η_ie) for the ultimate bearing capacity of a footing placed adjacent to a slope, taking into account the combined effect of horizontal and vertical seismic loads, represented by horizontal and vertical seismic coefficients, k_h and k_v, respectively, was derived using a modified Janbu's slice method. The influence of slope angles ‘α’ on the values of ‘η_ie’ are studied here. It was found that the values of η_ie can be expressed as an exponential function of ‘k_h/(-k_v)’ and ‘α’, with a measurable interdependency between ‘α’ and ‘η_ie’. The influence of ‘α’ on the value of ‘η_ie’ increases as the input value of ‘k_h/(-k_v)’ increases. Equations derived based on the analytical results are proposed to account for this effect. Based on the analyses of 11 near-fault seismographers obtained in the 1999 Chi-Chi earthquake in Taiwan, a ratio between the vertical and the horizontal seismic coefficients, λ, of between ±0.25 is suggested for including the combined effect of vertical and horizontal seismic forces in evaluating the seismic bearing capacity of footings located in near-fault areas.

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At present, analytical or empirical formula for seismic bearing capacity of footings adjacent to slopes is not available. This study uses a pseudo-static-based approach in conjunction with rigorous Janbu's slice method to derive analytical values of seismic bearing capacity factors (N_γ) and correction factors for the effects of inertia of soil mass and load inclinations for a rigid footing adjacent to cohesionless slopes. It is shown that both the bearing capacity factors (N_γ) and the correction factors for the seismic bearing capacity of footings placed on level ground derived herein are comparable with those reported in the literature. Empirical equations regarding the effects of slope angles and load inclinations, expressed using generalized forms of those proposed in the literature, are also derived. It is also found that the empirical equations derived in the present study provide values of correction factors in good agreements with the analytical ones, indicating the validity of using these empirical equations for assessing the bearing capacity of rigid footings situated on the slope subjected to pseudo-static seismic loading.

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 The stability of

‒tetrahydrocannabinol acetate (‒THC‒OAc) and ‒tetrahydrocannabinol acetate (‒THC‒OAc) in -liquid during storage was investigated. ‒THC‒OAc liquids in cartridges were stored at 80℃ or 30℃ for 28 days. The relative concentrations of cannabinoids in the liquids were measured by gas chromatography with flame ionization detection. ‒THC‒OAc decreased during storage at either temperature. ‒THC, a minor impurity, also decreased. ‒THC‒OAc liquid in a cartridge was stored at 80℃ for 57 days. The concentration of ‒THC‒OAc and ‒THC, a minor impurity, did not change during that time. Cannabinol acetate increased in all liquids, and unknown products were also detected by gas chromatography/mass spectrometry (GC/MS). The ‒THC‒OAc and ‒THC‒OAc liquids were subjected to GC/MS to detect representative diluents, glycerol, propylene glycol, and polyethylene glycol 400, but none of these were detected.

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The Gujarat earthquake in India occurred in January, 2001, and caused significant damage in the province of Gujarat. The Japanese Geotechnical Society sent a small reconnaissance team to the damaged region after the quake. The present text presents the report from this activity. The major attention of the team was focused on geotechnical aspects of the damage which were related to earthfill dams and harbor land fills. It was found that a significant portion of damage was concentrated in fills resting on soft natural soils. Swedish weight soundings which were conducted at two places demonstrated the existence of such a soft subsoil. From this, it was concluded that amplification of earthquake shaking as well as the permanent deformation in the soft foundation soil induced such kinds of damage as subsidence, cracking, and lateral spreading in overlying artificial fills. For the better seismic resistance of those affected fills during future earthquakes, the improvement of soft subsoil seems essential.

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The boundary element method expanded in frequency domains is presented to analyze the dynamic interaction between an embedded flexible rectangular foundation and soil with consideration of the obliquely incident waves. Numerical results describing the influence of the flexibility of the foundation on the dynamic responses of the foundation due to obliquely incident waves indicate that the flexibility of actual foundations can diminish the reduction of translation responses and increase the rotational responses in the high frequency range. These phenomena are more conspicuous as the embedment ratio is larger and the value of the wave velocity ratio of the soil and the foundation approaches to unity. When the high frequency components of the input ground motion are important and the basement has higher flexibility (for example ₂v_s/

1v_s

>0.

4

), the analysis method which considers the basement as a rigid foundation may lead to unsafety estimations and the estimation of the flexibility of the foundation is necessary as analysing the effective input motion with consideration of the incident waves.

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2-Benzyl--chloro--mercapto- (2H)-pyridazinone () was heated in ethanol under reflux for 10 hours to form concurrently 2, -dibenzyldipyridazo [, - : ', '-]-, -dithiin-, (2H, H)-dione (Ia) (57% in yield) and 2, -dibenzyldipyridazo [, - : ', '-]-, -dithiin-, (2H, H)-dione (IIa) (14% in yield). Assignment of the two products to the corresponding structures is established by their physico-chemical constants and chemical behaviors. The concurrent formation of the dipyridazo [, - : ', '-]-, -dithiin-, (2H, H)-dione and the -, (2H, H)-dione were observed in, not only heating -chloro--mercapto- (2H)-pyridazinones (-) in polar solvent, but warming -mercapto--chloro- (2H)-pyridazinones (-) in the presence of potassium carbonate in DMF. For the interpretation of the reaction, keto-thioketo carbenes as active intermediate species and a reversible interconversion among them are suggested on the basis of the fact that there was nonexistence of an equilibrium between the two compounds, such as Ia and IIa, under the reaction condition and a trapping keto-thioketo carbene species as 2-phenylimino--benzylpyridazo [, -d]-, -dithiol- (H)-one (IVa) (14% in yield) along with the major products, (Ia) and (IIa), was furnished by warming with phenylisothiocyanate in the presence of triethylamine in dry benzene. On the contrary, participation of a reversible interconversion between Ia and IIa, to a considerable extent, with the concurrent formation of them in the case of benzylation of either Ib or IIb, by warming with benzylchloride in the presence of potassium carbonate in DMF at 80°, might not be neglected, because an attempted approach to an equilibrium between Ia and IIa in a similar reaction condition except the use of benzylchloride realized, whereas non-existence of an equilibrium between Ib and IIb in the similar reaction condition was observed.

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