No abstract

A ring-opening reaction of cyclopropanes with five-membered heteroaromatics having a leaving group at C(2) was found to provide heteroaromatic-fused pyrrolidines in one step. This reaction was successfully applied to the synthesis of the protein kinase C-beta inhibitor JTT-010, which possesses a dihydropyrrolo[1,2-a]indole core.

The relationship between magnetic resonance (MR) relaxation times and muscle fiber composition was investigated in 16 men, and a high positive correlation was found. Higher proportions of fast-twitch fiber were associated with longer relaxation times, indicating that fast-twitch fiber has a longer relaxation time than slow-twitch fiber. Multiple regression analysis, conducted to investigate the suitability of relaxation time as a model of estimating muscle fiber composition, revealed that T1 and T2 were significantly related to muscle fiber composition. These results indicate that MR relaxation time may be used to estimate muscle fiber composition.

The effect of muscle hypertrophy on the relationship between magnetic resonance (MR) relaxation time and muscle fibre composition was investigated. Relaxation time and muscle fibre composition were measured in five subjects before and after a 20-week period of strength training. Muscle fibre composition in all subjects exhibited a significant shift to a predominance of fast-twitch (FT) fibres as a result of 20-week strength training (% area FT fibres: mean values from 49.8%, SD 17.9% to 57%, SD 5.6%; P less than 0.05). Longitudinal relaxation time (T1) and transverse relaxation time (T2) were prolonged significantly after strength training (T1 mean values from 334.9 ms, SD 13.6 to 359.0 ms, SD 9.0, P less than 0.001; T2 from 27.5 ms, SD 0.9 to 30.8 ms, SD 2.3, P less than 0.05). A constant relationship was observed in changes caused by strength training in muscle fibre composition (% area FT) and relaxation time, with a high correlation obtained between both parameters. These results indicate that MR relaxation time can be used for non-invasive estimation of muscle fibre composition.

This paper describes the optimum design methodology for improving operating characteristics of hydrodynamic journal bearings and its application to elliptical journal bearing design used in high-speed rotating machinery. The hybrid optimization technique combining the direct search method and the successive quadratic programming is applied effectively to find the optimum solutions. In the optimum design of elliptical journal bearings, the design variables such as vertical and horizontal radial clearances, bearing length-to-diameter ratio and bearing orientation angle are determined to minimize the objective function defined by the weighted sum of maximum averaged oil film temperature rise, leakage flow rate, and the inversion of whirl onset speed of the journal under many constraints. The results obtained are shown in graphical form for a wide range of journal rotational speed. Comparing the optimized operating characteristics with the characteristics calculated from the random selected design variables, the effectiveness of optimum design is clarified.