FutureChem (South Korea)

This study compared the effects of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) as 64Cu-chelating agents in newly developed prostate-specific membrane antigen (PSMA) target compounds, 64Cu-cudotadipep and 64Cu-cunotadipep, on pharmacokinetics. The in vitro stability of the chelators was evaluated using human and mouse serum. In vitro PSMA-binding affinity and cell uptake were compared using human 22Rv1 cells. To evaluate specific PSMA-expressing tumor-targeting efficiency, micro-positron emission tomography (mcroPET)/computed tomography (CT) and biodistribution analysis were performed using PSMA+ PC3-PIP and PSMA- PC3-flu tumor xenografts. The serum stability of DOTA- or NOTA-conjugated 64Cu-cudotadipep and 64Cu-cunotadipep was >97%. The Ki value of the NOTA derivative, cunotadipep, in the in vitro affinity binding analysis was higher (2.17 ± 0.25 nM) than that of the DOTA derivative, cudotadipep (6.75 ± 0.42 nM). The cunotadipep exhibited a higher cellular uptake (6.02 ± 0.05%/1 × 106 cells) compared with the cudotadipep (2.93 ± 0.06%/1 × 106 cells). In the biodistribution analysis and microPET/CT imaging, the 64Cu-labeled NOTA derivative, 64Cu-cunotadipep, demonstrated a greater tumor uptake and lower liver uptake than the DOTA derivative. This study indicates that the PSMA-targeted 64Cu-cunotadipep can be applied in clinical practice owing to its high diagnostic power for prostate cancer.

Abstract Natural polymers with abundant side functionalities are emerging as a promising binder for high‐capacity yet large‐volume‐change silicon anodes with a strong and reversible supramolecular interaction that originates from secondary bonding. However, the supramolecular network solely based on hydrogen bonding is relatively vulnerable to repeated deformation and has an insufficient diffusivity of lithium ions. Herein, reported is a facile but efficient way of incorporating the natural polymers with an ionically conductive crosslinker, which can construct a robust network for silicon anodes. The boronic acid in the crosslinker spontaneously reacts with natural polymers to generate boronic esters at room temperature without any kind of triggers, which gives a strong and dynamic covalent bonding to the supramolecular network. The other component in the crosslinker, polyethylene oxide, contributes to the enhanced ionic conductivity of polymers, leading to outstanding rate performances even at a high mass loading of silicon nanoparticles (>2 mg cm−2). The small portion of the proposed crosslinker can modulate the strength of the entire network by balancing the covalent crosslinking and self‐healing secondary interaction along with the fast lithium‐ion diffusion, thus enabling the extended operation of silicon electrodes.

Solvent effects on nucleophilic displacement reactions of alkyl mesylates with halide ions were investigated in a series of protic alcohol solvents. In consideration of Hughes and Ingold's principle, the reaction rates were found to correlate well with the normalized solvent polarities () in all halide reactions.

Abstract The highly regioselective and efficient synthesis of diverse substituted‐benzothiazoles, including heterocyclic units and amino groups, was achieved in moderate to high yields from ortho ‐bromothiobenzanilides, ortho ‐bromoarylthioureas, ortho ‐bromobenzanilides, and ortho ‐dibromobenzanilides, regardless of the electron density and substituted positions, via the prevalent carbon‐sulfur bond formation by thermally induced intramolecular cyclization reaction without using any metal sources or other additives. Polysubstituted‐benzothiazoles, particularly 2,4‐, 2,6‐disubstituted, and 2,4,6‐trisubstituted benzothiazoles, could be efficiently synthesized by a facile cascade reaction from appropriate ortho ‐bromobenzanilides under general thiolation conditions. This benign reaction represents a straightforward and practical approach toward diverse substituted‐benzothiazoles. In addition, the remaining bromine substituent of the resulting products was further utilized as a functional handle for the additional diversification and exploited as a complementary solution for the adjustment of harsh reaction condition. This methodology not only allows for the elaboration of benzothiazole molecules, but also provides a new valuable synthetic tool for a range of pharmaceutical applications.

To evaluate the efficacy of 18F-FC119S as a positron emission tomography (PET) radiopharmaceutical for the imaging of Alzheimer's disease (AD), we studied the drug absorption characteristics and distribution of 18F-FC119S in normal mice. In addition, we evaluated the specificity of 18F-FC119S for β-amyloid (Aβ) in the AD group of an APP/PS1 mouse model and compared it with that in the wild-type (WT) group. The behavior of 18F-FC119S in the normal mice was characteristic of rapid brain uptake and washout patterns. In most organs, including the brain, 18F-FC119S reached its maximum concentration within 1 min and was excreted via the intestine. Brain PET imaging of 18F-FC119S showed highly specific binding of the molecule to Aβ in the cortex and hippocampus. The brain uptake and binding values for the AD group were higher than those for the WT group. These results indicated that 18F-FC119S would be a candidate PET imaging agent for targeting Aβ plaque.

The objective of this study was to develop and evaluate the construct validity of a Nutrition Quotient (NQ) for children. In a previous report (Kang, et al., 2012), the food behavior checklist for children’s NQ, consisting of 19 items, was grouped into a 5-factor structure according to the exploratory factor analysis: balance, diversity, moderation, regularity, and practice. In this study, the construct validity of the NQ was assessed using a confirmatory factor analysis. Elementa ry school students (n = 1,393) from six large cities completed the NQ test. Indicator tests suggested an adequate model fit (goodness of fit index = 0.9613; adjusted GFI = 0.95; standardized root mean square residual = 0.0464; chi-square test statistics of ＜ 0.001 p-value, 82.1), and item loadings were significant for all subscales (p ＜ 0.05). The standardized path coefficients were used as the weights of the items. The NQ and the 5 factor scores of the student were calculated by the obtained weights of the questionnaire items. Logistic regression was applied to find the significant factors in order to af fect a specific nutrient status. The receiver operation characteristic curve analyses were performed in order to find diag nostic cut-off points of the five factors. The food behavior checklist for children’s NQ would be a handy and suitable in strument for evaluating dietary behaviors of Korean children. (Korean J Nutr 2012; 45(4): 390 ~ 399)