(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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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 activities of tobramycin derivatives acetylated and ethylated on the '-N, '-N and 3-N positions were examined. The MICs of these derivatives against tobramycin sensitive strains indicated that '-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 '-N or '-N ethylation protects the drug against inactivation by AAC(') or AAC('), respectively, and '-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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Two new polyacetylene compounds (, , 12)--acetoxy-3-isovaleryloxytetradeca-, , 12-trien-, 10-diyn-14-ol (), and (, , 12)--acetoxy-3-(-methylbutyryloxy)tetradeca-, , 12-trien-, 10-diyn-14-ol () have been isolated along with (, , 12)--acetoxy-3-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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Stress wave theory is applied to open-ended pipe piles to clarify the effects of soil plug on the behaviour of piles during driving and static loading. Measured field data and various numerical models are reviewed ; methods are presented to calculate wave propagation in both the pile and the soil plug ; modelling is presented which takes into account the interaction between the soil plug and the pile ; also presented is simplified method to estimate the loadsettlement relation of the pipe pile in static loading. By correlating observed and calculated values in two analytical cases, the authors demonstrate that incorporation of the soil plug (modelled as a series of masses and springs) is required to correctly predict pile behaviour during driving and static loading.

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

e

., - (, , , -tetrahydro-, , , -tetramethyl--naphthalenylcarbamoyl) benzoic acid (Am ) and () -- [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. μm Am , Ch 55 or RA for 96 h caused more than 90% suppression of -myc expression and around 10-fold increase in the percentage of NBT-positive cells.

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This study was performed to clarify which factors affected damage to tame-ike (small embankment dams for irrigation) in Hokudan Town as a result of the January 17, 1995 Hyogoken-Nambu earthquake. Factors were assumed to be : Location (.g., Distance to Epicenter, etc.), Structure (.g., Angle to Nearest Fault, Embankment Volume, etc.), Soil Properties of Embankment, Geology of Dam Site and History (Era of Construction, Repaired, etc.). Multivariate statistical analyses were performed for documentary data (damaged : 181, undamaged : 328). Ordinary statistical analyses were conducted for the data investigated in situ for soil properties of the embankment. The results show that the factors causing damage to dam are : () Nearest Fault (Nojima, Mizukoshi and D), () Distance to Nearest Fault (less than 500 m), (3) Distance to Epicenter (approximately to 14 km, which almost agrees with the location of seismic intensity JMA), () Elevation of Dam Site (higher than 100 m), () Embankment Volume (the greater the volume the more damage was caused), () Direction of Dam Axis (normal or diagonal to the epicenter or to nearest the fault), () Plan View of Dam Axis (3 or axes), () Surface Geology of Dam Site (non-cohesive soil type ground), () Era of Construction (prior to 1891) and (10) Soil Properties of Embankment (sand, not silty sand or gravel, penetration resistance that is 10% smaller than the undamaged dams).

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The syntheses of (S)-13-hydroxy-(, , )-tetradecatrienoic acid () and (, , Z-tetradecatrienoic acid () were carried out by using the Wittig reaction as the key step. The asymmetric center at -13 and the double bond between - and - for natural compound were reconfirmed as being of (S) configuration and , respectively. The relationship between the structure of the unsaturated hydroxy fatty acids and their inhibitory effect on the growth of lettuce was investigated.

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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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In the seismic analysis of pile foundations the soil is often assumed to be an elastic material and the pressure at the soil pile interface is not limited during the analysis. This may result in a considerable error, as the computed pressure from an elastic analysis may go well beyond the ultimate lateral pressure of real soil. In fact, significant yielding at the soil-pile interface has been observed during real earthquakes, and also in laboratory tests. The yield zone is usually near the ground surface where the effect of inertial force due to the superstructure is higher. This yielding redefines the pile response, and in general cannot be ignored. In order to examine the effects of soil yielding on the internal pile response during earthquakes an approximate analysis is described in this paper which is an extension of a static method developed by the second author (1982) for the analysis of piles subjected to lateral soil movement. This method is then used to investigate the effects of soil yielding on the internal response of piles through a comparative study in which real earthquakes are used. It is shown that for strong earthquakes and heavily loaded piles the soil yielding may considerably increase the amount of maximum pile moment developed in the pile. A marked difference in the effects of yielding on the pile moment and shear is observed and discussed.

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The interaction between a penetrating shaft and the surrounding soil media under impact loading is a frequently encountered phenomenon in geotechnical engineering. Examples of such dynamic soil/shaft interaction would include dynamic pile driving, standard penetration testing (SPT), and dynamic driven rod test. Presented in this paper is a novel approach, based on the principle of dynamic system identification, which enables identification of dynamic soil-pile interaction model parameters. The analytical transfer function, relating the output stress wave forms to the input stress wave forms in the soil/shaft system, is derived using the Laplace and Fourier Transform techniques and the one-dimensional wave propagation theories. A numerical solution algorithm based on a variation of gradient method is coded into a micro-computer based program to solve the frequency-dependent soil-pile interaction parameters (Smith model) : soil damping and soil spring stiffness. To further reduce the amount of computational effort required in the solution of the frequency-dependent dynamic soil properties, it is suggested that the solution be obtained for the first-mode natural frequency of the measured stress waves. The results obtained from this simplified solution algorithm, when compared with both numerical simulations and controlled laboratory tests, are reasonably acceptable. The proposed parameter identification technique offers a viable alternative data interpretation procedure for deducing pertinent Smith model parameters used frequently in pile driving analysis.

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  The distribution of sarcophytol-A in the Sarcophyton genus was investigated in seven samples belonging to S. glaucum (3 samples), S. infundibulifurme ( samples), S. crassocaule ( sample) and S. trocheliophorum ( sample) that were collected on Ishigaki Island in Okinawa Prefecture. Sarcophytol-A was present in one sample each of S. glaucum and S. infundibulifurme. This study indicates that the composition of cembranoids in the Sarcophyton genus is not related with the respective species, but with the individual samples collected.

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-Benzyl--chloro--mercapto-3 (H)-pyridazinone () was heated in ethanol under reflux for 10 hours to form concurrently , -dibenzyldipyridazo [, - : ', '-]-, -dithiin-, (H, H)-dione (Ia) (57% in yield) and , -dibenzyldipyridazo [, - : ', '-]-, -dithiin-, (H, 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-, (H, H)-dione and the -, (H, H)-dione were observed in, not only heating -chloro--mercapto-3 (H)-pyridazinones (-3) in polar solvent, but warming -mercapto--chloro-3 (H)-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 -phenylimino--benzylpyridazo [, -d]-, 3-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 °, 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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Natural sedimentary clays exhibit ageing effects on their behaviour when subjected to both consolidation and shearing. Attempts to characterising the in-situ 'structure'of soft marine clays have been made in case studies performed in Ariake (Japan) and in Bangkok (Thailand), each showing a typical profile of aged clay-structure with depth reflecting its site-specific geological consolidation history. In each site, profiles of Atterberg limits, natural water content, overconsolidation ratio (OCR), quasi-elastic shear modulus G_max and the undrained shear strength c_u with depth were attained from various laboratory tests, together with the a comparable profile of quasi-elastic shear modulus from insitu seismic survey G_f. Quantitative assessment of the aged clay-structure was made by using two different measures, metastability index MI (G) and the soil constant reflecting structure S (Jamiolkowski et al., 1994). The profiles of MI (G) and the S-value with depth were both determined based on the corresponding G_max behaviour of the reconstituted sample. "Disturbance"of laboratory samples retrieved by using two different samplers (i.., Laval and Japanese thin-walled samplers) with two different sampling techniques (i.., pre-boring and displacement methods) was discussed. A new approach to estimate c_u"in the ground", termed by the authors the MILK (Metastability Index coupled with Laboratory K_o test) method, is proposed. A trial of the MILK-method is demonstrated in soft Bangkok clay, the texture of which is similar to "soft cheese".

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In view of the significant role of the water film effect in flow failure for a liquefied sandy deposit, the mechanism of water film generation is numerically studied based on a -dimensional model test. The process of water film growth and decay can be simulated to a certain extent by a simple consolidation analysis, which indicates that only a small difference in permeability in layered sand is enough for a water film to develop. A G shaking table test for a two-dimensional slope model with an arc of silt within a saturated sand is then addressed to discuss the dilatancy effect exerted in sheared sand during flow failure. It is possible that, once the water film is formed, the transmission of shear stress through it is interrupted, leaving the sand below free from the dilatancy ; this eventually allows the water film to stay without being absorbed during flow failure. The result of another shaking table test for a trapezoidal slope with horizontal silt seams indicate that water films beneath the seams enable the soil mass above them to laterally flow along water films very gently inclined even after shaking. If a silt seam breaks due to excessive pressure in the water film, it triggers re-liquefaction in the upper sand and leads to further instability.

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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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