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It is known that thiazolo[3,2-a][1,8]naphthyridine derivatives (3a) exhibit good antibacterial activity. Accordingly, several analogues of 3a, viz. oxazolo- and imidazolo[3,2-a][1,8]naphthyridine derivatives 3b and 3c, were synthesized and evaluated for antibacterial activity in vitro and for inhibitory activity against DNA gyrase of Escherichia coli K-12 C600. Compound 3a exhibited antibacterial activity comparable to that of ofloxacin and enoxacin against Gram-positive and Gram-negative bacteria and displayed antibacterial activity superior to that of 3b and 3c. The antibacterial activities of 3b and 3c decreased in that order. DNA gyrase inhibitory activities of 3a-c in E. coli K-12 C600 paralleled their in vitro antibacterial activity. It was found that enhancement of the DNA gyrase inhibitory activity of 3a was dependent on a certain feature of the sulfur atom of the thiazole ring.

BackgroundThe purpose of this study was to clarify the characteristics of body composition and cardiometabolic risk of Japanese male heavyweight Judo athletes compared with heavyweight athletes of other sports.MethodsNineteen heavyweight Judo athletes (mean age, 20.4 ± 1.1 years), as well as 22 heavyweight (mean age, 21.5 ± 0.9 years) and 17 nonheavyweight (mean age, 21.1 ± 0.8 years) American football and Rugby football athletes in Japan participated in this study. Body composition was assessed by using dual-energy X-ray absorptiometry and magnetic resonance imaging. Cardiometabolic risk was evaluated by measuring blood biochemical variables.ResultsHeavyweight Judo athletes had significantly heavier body mass (122.7 ± 13.1 kg vs. 99.0 ± 8.1 kg), higher body fat percentage (27.5 % ± 5.2 % vs. 19.4 % ± 4.7 %), and larger visceral fat cross-sectional area (118 ± 35 cm2 vs. 67 ± 24 cm2) (P < 0.01) compared with heavyweight football players. Although the cardiometabolic risk was higher in heavyweight athletes compared to nonheavyweight athletes, there were no significant differences between heavyweight Judo and heavyweight Football athletes in the blood biochemical variables, except for high concentration of uric acid in heavyweight Judo athletes.ConclusionsEven though heavyweight Judo athletes had more excess fat mass, especially VF mass, their cardiometabolic risk in terms of blood biochemical parameters was not significantly higher compared with heavyweight athletes of other sports. Therefore, excessive fat accumulation may not necessarily increase cardiometabolic risk for heavyweight Judo athletes.Trial registrationThis trial is registered with the University Hospital Medical Information Network Clinical Trial Registration (UMIN-CTR) UMIN000020564.

The crystallization behavior of drugs from supersaturated solutions containing carboxymethylethylcellulose(CMEC)was investigated to clarify the mechanism of supersaturation phenomena from solid dispersions with enteric coating agents in JP XI 2nd fluid(pH 6.8). Nifedipine,griseofulvin and spironolactone were used as drugs.The rate of crystallization of all drugs was remarkably inhibited by the presence of CMEC.It was found that the inhibition was not due to solubilization of the drugs by CMEC. The crystallization kinetics from supersaturated solutions suggested that the process of crystal growth itself was directly inhibited.Physical properties of the crystallized mass were also investigated in the case of nifedipine.It was thought that the inhibitory effect of CMEC on the drug crystallization was due to the adsorption of CM EC at the solid-water interface at the stage in which a hydrophobic drug crystal surface was formed,and further drug molecules could not deposit easily on the crystal surface for the following reasons;(1)formation of a step or kink,which is necessary for the crystal growth,was inhibited by polymer adsorption,and(2)molecular diffusion to the crystal surface was inhibited by the adsorbed polymer.Keywords-nifedipine;griseofulvin;spironolactone;solid dispersion;supersaturation;crystallization;crystal growth Chiou and Riegelman defined a "solid dispersion" as a dispersion of one or more active ingredients in an inert carrier or matrix in the solid state prepared by the melting(fusion), solvent,or melting-solvent method.2)It is well known that many drugs in solid dispersions are present as a high-energy amorphous phase and a solid dispersion using a water-soluble carrier shows supersaturation of a poorly soluble drug when the system is added to an aqueous medium.3)It can be considered that the dissolution of the drug takes place in the solid state prior to its exposure to the liquid medium.2) A few investigators have examined the dissolution mechanism of solid dispersions.4) However,quantitative analysis of the dissolution behavior in the amorphous state is quite difficult,since the amorphous state does not possess heat of fusion or solution,and this state transforms to the stable crystalline form easily during the experimental period.We attempted to apply a solid dispersion technique using different types of enteric coating agents as inert carriers to control the absorption behavior of water-insoluble drugs.5) Most of the drugs in these solid dispersions were amorphous,and the dissolution of the solid dispersions was practically nil in JP XI 1st fluid(JP XI disintegration medium,pH 1.2). However,they dissolved rapidly in JP XI 2nd fluid(JP XI disintegration medium,pH 6.8)and showed supersaturation phenomena.We also investigated the crystallization behavior of nifedipine(NP)from supersaturated solutions containing various polymers,6)since it was

Summary Energy requirements can be estimated from resting energy expenditure (REE). However, little is known about factors influencing REE in Japanese female athletes. This study was performed to evaluate the relationship between REE and body composition in Japanese female athletes with a wide range of body sizes. Ninety-three athletes (age 20.3 Ϯ 1.2 y, height 162.8 Ϯ 6.4 cm, body weight (BW) 57.0 Ϯ 9.2 kg, fat-free mass (FFM) 45.4 Ϯ 6.2 kg) were classified into three groups according to BW: small-size (S) ( n ϭ 34), medium-size (M) ( n ϭ 34), and large-size (L) ( n ϭ 25). Systemic and regional body compositions (skeletal muscle (SM), fat mass (FM), bone mass (BM), and residual mass (RM)) were estimated by dual energy X-ray absorptiometry (DXA). Measured resting energy expenditure (REEm) was evaluated by indirect calorimetry. Marked differences were found in REEm (S: 1,111 Ϯ 150, M: 1,242 Ϯ 133, L: 1,478 Ϯ 138 kcal/d), and systemic and regional body compositions among the three groups. REEm was strongly correlated with FFM, and absolute values of RM and SM increased significantly according to body size. There was good agreement between REEm and estimated REE (REEe) from the specific metabolic rates of four major organ tissue level compartments. These data indicate that REE for female athletes can be attributed to changes in organ tissue mass, and not changes in organ tissue metabolic rate. That is, change in REE can be explained mainly by the change in FFM, and REE can be assessed by FFM in female athletes regardless of body size. Key Words female athletes, resting energy expenditure, body composition, body size, fatfree mass Energy balance is a primary concern in most female athletes. Much of the effort of training can be lost when energy intake is insufficient to match that expended, as both body fat and body protein will be used for energy. In addition, if energy intake is limited or restricted, the ability to obtain other essential nutrients necessary for optimal sport performance and good health will be compromised. Previous studies suggested that chronic energy deficit have been implicated in health problems of female athletes such as disturbance of menstruation, osteopenia, eating disorders and anemia ( 1-3 ). Therefore, it is essential to properly manage the energy intake matched with energy requirement in female athletes.Energy requirement can be estimated from resting energy expenditure (REE). Estimated energy requirement (EER) is calculated using the estimation equation based on REE in the Dietary Reference Intakes for Japanese, 2010 (DRIs) ( 4 ). In most sedentary healthy adults, REE accounts for approximately 60% of total daily energy expenditure ( 5-7 ). It is well documented that REE is influenced by age, sex, body size, and body composition, including an individual's fat-free mass (FFM) or fat mass (FM) ( 8-10 ). In fact, these factors are usually included in prediction equations for REE ( 9 , 11 , 12 ), and three of these variables (age, sex, and FFM) generally account for 80% of the variabili...