4-Substituted-5(3)-carbamoyl-3(5)-(2-deoxy-β-D-ribofuranosyl)pyrazoles. Application of Palladium Catalyzed Glycal Coupling Methodology to the Synthesis of Pyrazofurin Analogs

Abstract

Analogs of the C-nucleoside pyrazofurin were prepared in 7–9 steps using a key Pd(0)- catalyzed coupling reaction between protected iodopyrazoles 6a and 6b and glycal 8 to form the glycosyl bond. Conditions for this reaction were improved from those previously described for related reactions in order to maximize product yields and eliminate the need for triphenylarsine.

     

Stereocontrolled Transesterification for the Synthesis of Chiral Phosphite Triester Backbone

Abstract

We have developed stereocontrolled transesterification for the synthesis of chiral phosphite mester backbone under basic conditions. Substrate phosphite triesters with phenoxy derivative substituents as leaving groups were separated into individual stereoisomers and reacted with hydroxyl-containing compounds to form desired backbone.

     

Geographical shift of zooplankton communities and decadal dynamics of the Kuroshio–Oyashio currents in the western North Pacific

We investigated temporal and spatial variations in the zooplankton community structure in the Oyashio and Transition region of the subarctic western North Pacific from 1960 to 1999 using principal component analysis (PCA) and zooplankton samples from the historical Odate Collection. In particular, we examined the influence of Kuroshio and Oyashio decadal dynamics on geographical variations in the zooplankton community. The first principal component (PC1) closely represented the interannual variation in cold-water, large copepod species, while the second PC (PC2) represented the variation in warm-water, small copepod species. Using Rodionov's regime-shift method, we detected a significant increase in the PC score after 1976 and 1981 for PC1 and PC2, respectively. After the shift years, (1) warm-water species increased in the Transition zone, (2) the distribution center of the cold-water species shifted southward, and (3) copepod abundance and species diversity increased in the Transition zone as a result of (1) and (2). The timing of these shifts in the zooplankton community roughly coincided with the North Pacific climatic regime shift in 1976/1977. From the mid-1970s to the early 1980s, the southern boundary of the Oyashio shifted southward and increased geostrophic transport was observed in the Kuroshio, indicating spin up of the Kuroshio–Oyashio system. Change in atmospheric circulation during the 1976/1977 regime shift is thought to have caused the spin up of these currents, which subsequently affected the regional zooplankton community through advective processes.     

Some Reactions of 4′-Thionucleosides and Their Sulfones

Abstract

We report interesting and novel reactions of 4′-thionucleosides and their sulfone derivatives when a good leaving group is present in the 5′-position. The results have important implications for the phosphorylation of these nucleoside analogues by standard chemical procedures. Possible mechanisms for these reactions are discussed.

     

Post introductory risk assessment studies on Zygogramma bicolorata (Coleoptera: Chrysomelidae), a classical biological control agent of Parthenium hysterophorus (Asteraceae) in India

Zygogramma bicolorata Pallister (Coleoptera: Chrysomelidae), a biological control agent of Parthenium hysterophorus L. (Asteraceae), was feeding on leaves of Helianthus annuus in India, raising concerns of its host range. Based on the age grading technique, it was shown that the majority of Z. bicolorata on sunflower plants at any time were reproductively immature. This establishes that Z. bicolorata does not pose any risk to sunflower in India.     

Detection and Prediction of Tooth Mobility During the Periodontitis Healing Process

The focus of the article is on a generic approach to prediction of a healing process based on automatic measurement and modelling of mechanical disease indicators. As a specific example the healing process after treatment of advanced periodontitis is characterised and predicted based on measurement of tooth mobility (TM). For the measurement a new mechatronic instrument was developed that includes a pneumatically driven probe with incorporated sensors of tooth displacement and loading force. TM is measured by a computer controlled data acquisition system and predicted by a non-parametric regression. Similarly as in the characterisation of technical processes, a measured sample is described by TM time series detected on a particular patient, while the regression is determined by a set of samples obtained from a group of patients following periodontal therapy. The influence of surgical access therapy and systemic administration of metronidazole as an adjunct to the mechanical treatment is demonstrated. For this purpose the average changes of tooth mobility are determined on variously treated subgroups. A new method of healing process prediction is demonstrated and its performance is described by a prediction quality.     

Aldolase and Actin Protect Rabbit Muscle Lactate Dehydrogenase from Ascorbate Inhibition

Muscle-type LDH (LDH-m4) activity is critical for efficient anaerobic glycolysis. The results here show that rabbit LDH-M4 is inhibited by concentrations of ascorbate normally found in tissues. Aldolase and muscle G-actin were found to protect and to reverse inhibitions of LDH-m4 by ascorbate. G-actins showed some species specificity. Myosin, tropomyosin and troponin from rabbit muscle and muscle proteins from other animal sources had no affect on the inhibitions by ascorbate. The substrate inhibition of LDH-m4 by pyruvate is partially relieved by the presence of aldolase and lowers the Km without affecting the Vm. G-actin under similar conditions has no affect. It is believed that these studies reflect some of the resting properties of glycolytic enzymes that bind and unbind to contractile elements. It is proposed that ascorbate facilitates the storage of glycogen in muscle at rest by inhibiting glycolysis.     

THE OCCURRENCE OF HISTOCHEMICAL ACTIVITY OF 3β-HYDROXYSTEROID DEHYDROGENASE IN THE DEVELOPING TESTES OF POECILIA RETICULATA

In the mature testes of the guppy, Poecilia reticulata , some groups of cells, distributed sparsely in the interspace between the peripheral germ cell layer and the hilar duct system, show evident histochemical response for Δ⁵-3β-hydroxysteroid dehydrogenase (3β-HSD). In the testis of newly delivered guppies, somatic cells are present in the testicular hilus as a compact mass without revealing any structural differentiation. In the testis of juvenile fish of the 8mm stage about 7 days after birth, interstitial cells resembling histologically those of adult testes become differentiated from the somatic cell mass and, though only in some specimens, coincidentally begin to display weak but obvious histochemical response for 3β-HSD. Thereafter the occurrence of enzyme activity becomes increasingly regular in the developing testes, and attains the adult pattern of distribution in testes of all specimens after the 11 13mm stage or 17 ∽ 20 days of age.
The appearance and enhancement of 3β-HSD activity in the testis is concurrent with the differentiation and development of the testicular duct system. Treatments of newly delivered fish with methyltestosterone (30 ∽ 50 μg/g diet) distinctly stimulate the development of the duct system, which suggests a possible role of androgen secretion occurring in the early phase of the testicular development in the control of testicular organogenesis in the guppy.