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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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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(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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This study aimed to determine the prevalence of fecal carriage of extended spectrum β-lactamase (ESBL) and/or plasmidic AmpC β-lactamase (pAmpC) producing Escherichia coli among dogs (n=428) in Turkey. Polymerase chain reaction (PCR) and sequencing were used to characterize genes encoding β-lactamase and plasmid mediated quinolone resistance (PMQR). Antimicrobial susceptibility testing and PCRs for virulence genes and phylogenetic groups were also performed. Cefotaxime resistant

. coli isolates were detected in 95 (.%) of the swab samples. Sequencing analysis results showed occurrence of various β-lactamase genes: bla_CTX-M-15 (62), blaTEM-

1b

(42), blaCMY-

2

(

22

), bla_CTX-M-3 (16), bla_CTX-M-1 (15), bla_OXA-1 (9) and bla_SHV-12 (3) alone or in combination. The most frequently encountered phylogenetic group was group A₁ (35.

8

%), followed by group

D₂

(

22

.1%),

B

1 (15.

8

%), D₁ (9.5%), A₀ (7.

4

%),

B2₂

(5.3%) and

B2₃

(

4

.

2

%), respectively. PMQR genes, aac(6’)-Ib-cr, qnrS1 and qnrB10 were detected in 25.3, 10.5 and 1.1% of the isolates, respectively. While all isolates were susceptible to imipenem and amikacin, resistance rates to non-β-lactam antibiotics ranged from 20.0% for tobramycin to 56.

8

% for tetracycline. The virulence genes were only detected in 34 (36.

2

%) of the isolates and this isolates carried single or various combination of virulence genes of iucD, papC, papE,

f17a

-A and eaeA. Four isolates were identified as human virulent pandemic CTX-M-15 producing

E

. coli clone O25

b

:ST131/

B

2

. To the best of our knowledge, this is the first study to show fecal carriage of ESBL/pAmpC type β-lactamase producing

E

. coli isolates among dogs in Turkey.

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The syntheses of (S)-13-hydroxy-(, , )-tetradecatrienoic acid (1) and (, , Z-tetradecatrienoic acid () were carried out by using the Wittig reaction as the key step. The asymmetric center at C-13 and the double bond between C- and C-9 for natural compound 1 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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Six new cembranoids sarcophytol P (3), R (), S (5), K (), (11), and T (13) were isolated from the soft coral Sarcophyton glaucum. Sarcophytol P (3) was shown to be the 20-hydroxy derivative of the major component sarcophytol A (1), and afforded the cyclization product 6 in CHCl_3 at room temperature, in a same way as in 1. Sarcophytols R () and S (5) were correlated to 1, by conversion of its 7R,R and 7S,S epoxide derivatives. Sarcophytol K() was a 13, 14-dihydroxycembranoid having a 1,3Z-diene moiety. The absolute configuration of and its 1Z,3- and 1Z,3Z-isomers sarcophytol () and J (10) were determined by circular dichroism study of their bis-p-dimethylaminobenzoate derivatives. Sarcophytols (11) and T (13) were 1- and 1,3Z-isomers of 1. Compound 11 showed characteristic broadening of the ^1H-NMR chemical shifts, due to the restricted conformational interconversion. Using the three cembranoids sarcophytols (11, 1,3), N (15, 1Z,3Z) and T (13,1,3Z), spontaneous autoxidation-cyclization, in CHCl_3,was examined, in order to compare the stereochemical course of the reaction with that of 1 (1Z,3), which affords trans-fused bicyclo[9.3.0]tetradecene systems. The 1,3Z-isomer 13 gave the same cyclization product 18, as in the reaction of 1, even though it is isomeric at C-1,3. The 1Z,3Z isomer 15 gave 19, in consequence of the reversed geometry at C-3 of 15. The 1,3-isomer (11) gave the bicyclic product , having an antipodal fusion as compared with 19. This was confirmed by PCC oxidation of 19 and , giving enantiomeric ketones 23 and 24 respectively. The 1(14)-epoxide 26 was shown to be the immediate precursor of , and acounted for the inversion of the geometry at C-1 of the cyclization product. Compound 26 is isomeric with the epoxide 17 derived from 1. The epoxide 17 is the postulated precursor in the conversion of 13 to 18. It is noteworthy that the mode of antipodal fusion of the cyclopentane rings, in 18 and , was controlled by the chirality of the epoxy rings. The C-14 hydroxyl group participates in the transannular cyclization, but was found not to be the requisite functional group for the reaction. Similar treatment of cembrene C (30), the parent hydrocarbon of 1, also reacted in CHCl_3 giving the bicyclic product 32.

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Es geht Zuerst in dieser Abhandlung um eine strukturelle Analyse von sog. Hebammenperikope (Ex. 1; 15-), die gemeint ist, in dem zweite Buch Mose eine Kleine Einheit zu bilden, und danach motivgeschichtliche Untersuchung.
Erstens analysieren wir grammatisch den gegebenen Text: wie folgt, 1) Verse von 16 bis 19 entstehen aus drei “wayyo'mer + wörtliche Rede”, durch die in dieser Perikope dramatische Höhepunkt ausgedrückt wird. ) Bei der Korrelation von Verben, deren Subjekt Hebammen ist, und Verben, deren Subjekt König ist, hat sich herausgestellt, daß die Handlungen der Hebammen vielseitig sind, während die des Königs auf einigermaßen einseitigen Bereich weisen. 3) v. 21a ist im Hinblick auf die Satzbildung v. 17a ähnlich, obwohl jener für v. 21, der die Mehrung des Volkes beschreibt, nur einleitende Vers ist. ) Der Unterschied von mwt (töten) in v. 16 und šlk (werfen) in v. ist entscheidend; denn šlk betont hay^e' orah (in den Fluß).
Zweitens müssen wir Erzählungselemente dieser Perikope beschreiben: wie folgt, a) Namen der Hebammen (v. 15), ) Verlangen des Königs (v. 15a, 16), c) Gottesfrucht als Begründung (v. 17a), d) Ausweichen der Hebammen (17bc), ) Befragung des Königs (v. 18), ) Ausrede der Hebammen (v. 19), g) Wohlsein der Hebammen (v. 20a), h) Volksverstärkung (v. 20, 21), i) Ankündigung (v. ).
Nun drücken {, d, , , g, i} die Funktionen der Charaktere dieser Erzählung aus. Und zwar bezeichnet die Gegenüberstellung von oder diejenige von ein Funktionpaar, und g zeigt Endfunktion. {/d, /, g} bilden Einheit; folglich ist {i} die andersartige Funktion, die die anfängliche Situation der folgenden Geburtserzählung Moses (Ex. ; 1-10) bestimmt. Und wir nehmen diese sechs Funktionen als unveränderliche Zahlen an.
Volksverstärkung (h) deutet die Folge (↓) an, die das Ausweichen der Hebammen gewann, und gibt zugleich dem König Anlaß (↑) zur Ankündigung. Daher legen wir h für das Verbindungsmoment aus, das {/d, /, g} mit {i} verbindet. Dazu ist c beweglichste Element, das Erzähler gegen ein andre Element leicht auswechseln kann. Element a (Namen der Heldinnen), das nicht immer für die Entwicklung der Hebammenerzählung wesentlich ist, zeigt veränderliche Zahl.
Die Erzählung {/d, /, g} thematisiert die Weisheit von Hebammen. Wenn Elemente c and a dieser Erzählung eine spezielle Nuance geben, dann thematisiert die Hebammenerzählung die Gottesfrucht von Heldinnen.
Aus dem, was wir oben gesagt haben, läßt die Struktur dieser Erzählung sich schematisieren: wie folgt, a+c {/d, /, g} ↓ h ↑ {i}.
Drittens Können wir in der Verkündigung der Gottesfrucht ein ganz außergewöhnliches Anliegen des Elohisten () erblicken. Daher gehört Element c (Begründung), dessen Leitwort yr' (fruchten) ist, zu der Quellenschicht . Nebenbei gesagt, begegnet Wortpaar rbh-'sm nicht allein beim Verbindungsmoment h, sondern auch bei der Abrahamsüberlieferung usw. Es ist uns jedoch unmöglich, es auf bestimmte Quellenschicht festzusetzen.

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市販食用緑色3号(主色素:HSBA-(m-EBASA)(m-EBASA)、m,m-G-3)に含まれる3付随色素(Sub-A、、)を精製単離し、MSおよびNMRを用いて構造決定した。Sub-Aは主色素のエチル基の一つが脱離した化合物HSBA-(m-BASA)(m-EBASA)、Sub-はp,p-G-3、Sub-はo,p-G-3であった。以前報告した付随色素(Sub-C、、G、H)を含め、7つの付随色素の市販品(1社製品)中の含量を測定したところ、色素中にSub-Aは0.45〜1.20%、Sub-は0.19〜.60%、Sub-Cは.49〜27.0%、Sub-は0.05〜1.52%、Sub-は1.15〜.37%、Sub-Gは0.05〜0.%、Sub-HはND〜0.24%含まれていた。

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Tosylmethyl isocyanide () reacted readily with azole carbaldehydes, i.., indole--carbaldehyde (a), pyrazole-3 (5)-carbaldehyde (), 3 (5)-methylpyrazole-5 (3)-carbaldehyde (c), 3 (5)-(-furyl) pyrazole-5 (3)-carbaldehyde (d), 1, , -triazole-3 (5)-carbaldehyde (), and tetrazole-5-carbaldehyde (), in the presence of an equimolar amount of potassium carbonate in refluxing methanol to yield the corresponding 5-substituted oxazoles (10 and 15-) as the final products. In the case of the reaction of with imidazole--carbaldehyde (g), however, N-(1-tosyl-1-alkenyl) formamide of type 18g, 1-amino-1-tosyl--alkene of type 19g, and 3-tosylimidazo [1, -c] pyrimidine (g) were obtained, depending on the reaction conditions.

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The activities of tobramycin derivatives acetylated and ethylated on the 6'-N, '-N and 3-N positions were examined. The MICs of these derivatives against tobramycin sensitive strains indicated that '-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 '-N or 6'-N ethylation protects the drug against inactivation by AAC(') or AAC(6'), respectively, and '-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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Two effective cytochrome P450 (CYP) inhibitors were isolated from tarragon, Artemisia dracunculus. Their structures were spectroscopically identified as ,-undeca-,-diene-,10-diynoic acid isobutylamide (1) and ,-undeca-,-diene-,10-diynoic acid piperidide (). Both compounds had dose-dependent inhibitory effects on CYP3A activity with IC₅₀ values of 10.0 ± 1.3 µM for compound 1 and 3.3 ± 0. µM for compound , and exhibited mechanism-based inhibition. This is the first reported isolation of effective CYP inhibitors from tarragon (Artemisia dracunculus) purchased from a Japanese market.

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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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