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 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 (700–1,500 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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(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 6'-N, 2'-N and 3-N positions were examined. The MICs of these derivatives against tobramycin sensitive strains indicated that 2'-N-ethylated and 6'-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 6'-N ethylation protects the drug against inactivation by AAC(2') or AAC(6'), respectively, and 2'-N-ethyltobramycin and 6'-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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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 -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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A biosynthetic pathway for (

)-methyl cinnamate formation was evaluated in Tricholoma matsutake by tracer experiments using

13C

- and ²H-labeled precursors. One hundred percent selective

13C

incorporation was observed when L-[1,2,3,

4

,

5

,6,

7

,

8

,

9

-

13C₉

, ^15/N]phenylalanine was converted to (

E

)-[1,2,3,

4

,

5

,6,

7

,

8

,

9

-

13C₉

]cinnamate and (

E

)-[1,2,3,

4

,

5

,6,

7

,

8

,

9

-

13C₉

]methyl cinnamate. Similarly, 100% selective

13C

incorporation was observed when (

E

)-[1,2,3,

4

,

5

,6,

7

,

8

,

9

-

13C₉

]cinnamate was converted to (

E

)-[1,2,3,

4

,

5

,6,

7

,

8

,

9

-

13C₉

]methyl cinnamate. In contrast, the ²H incorporation selectivities were

82

.1% and

81

.

4

% when L-[2,3,

4

,

5

,6,

7

,

7

,

8

-

2H₈

]phenylalanine was converted to (

E

)-[2,3,

4

,

5

,6,

7

,

8

-

2H₇

]cinnamate and (

E

)-[2,3,

4

,

5

,6,

7

,

8

-

2H₇

]methyl cinnamate, respectively. Thus, T. matsutake synthesizes (

E

)-methyl cinnamate from L-phenylalanine via (

E

)-cinnamate. (

E

)-cinnamate was likely formed through two pathways: one was major and the other was a minor.

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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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The behavior of the soft clay grounds subjected to repeated loading is different from that subjected to sustained loading. The difference in settlement between these two loading patterns should be due to secondary compression over a long period of time. Consequently, soft clay grounds subjected to repeated loading tend to be more compressible than those subjected to sustained loading. Therefore, it is necessary for engineers to predict post-construction settlements under repeated loading. In this respect, the preloading is considered to be promising as a countermeasure to reduce the settlement of clay under repeated loading as well as under sustained loading. The effect of preloading on post-construction consolidation settlement of soft clay subjected to repeated loading after removal of a part of preload is investigated in the present paper. It has become clear that the settlement of a clay sample after preconsolidation is mainly affected by the amount of preload, the degree of consolidation due to the preload, the amount of permanent load and the amount of repeated load after removal of preload. The calculated settlement versus time relations using a method to estimate the amount of consolidation settlement of soft clay grounds subjected to repeated loading after removal of preloading were compared with the observed degree of consolidation as parameters of the intensities of preload and repeated load.

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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 1-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 1 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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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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Nine isoquinoline alkaloids belonging to the protoberberine, proaporphine and bisbenzyl-isoquinoline series were isolated from Caryomene olivascens (Menispermaceae). Four compounds are new : (-)-2-norlimacine (), (-)-caryolivine (6), (+)-1, 2-dehydro-2-norlimacusine () and N-formylstepharine (3). The last one is the first N-formyl derivative to be reported in the proaporphine group. Its biogenetic origin is discussed. Structures were established on the basis of 360 MHz (FT) nuclear magnetic resonance measurements and also by chemical correlation in the case of 3.

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2-Benzyl--chloro--mercapto-3 (2H)-pyridazinone (1) was heated in ethanol under reflux for 10 hours to form concurrently 2, -dibenzyldipyridazo [, - : ', '-]-1, -dithiin-1, 6 (2H, H)-dione (Ia) (57% in yield) and 2, -dibenzyldipyridazo [, - : ', '-]-1, -dithiin-1, (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 [, - : ', '-]-1, -dithiin-1, 6 (2H, H)-dione and the -1, (2H, H)-dione were observed in, not only heating -chloro--mercapto-3 (2H)-pyridazinones (1-3) in polar solvent, but warming -mercapto--chloro-3 (2H)-pyridazinones (-6) 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]-1, 3-dithiol- (H)-one (IVa) (14% in yield) along with the major products, (Ia) and (IIa), was furnished by warming 1 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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Two new partially saturated tricyclic ring systems, 6, 6a, , , , 10, 10a, 11-octahydro-11-oxodibenz [, ] oxepins (3a and 3), 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-d₆ (12). The stereochemical features of 3a (trans), 3 (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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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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