Fuji Chemical Industries (Japan)

The novel LpxC inhibitor T-1228 is a candidate drug molecule for multidrug-resistant Gram-negative bacterial infection. This report describes the synthesis of the diol unit of T-1228, (S)-1-(4-ethynylphenyl)ethane-1,2-diol, from commercially available 2-bromo-1-(4-iodophenyl)ethan-1-one, achieved in 5 steps and 4 isolations. The stereogenic center of the diol unit was created by means of a highly scalable form of the Corey–Bakshi–Shibata reduction; process parameters were optimized using the Design of Experiments methodology. Using this newly developed process chemistry route, we successfully synthesized 12.5 kg of (S)-1-(4-ethynylphenyl)ethane-1,2-diol in 60% total yield and optical purity >99% ee.

Introduction:This study aimed to determine the effect of preoperative variables and three-dimensional acetabular correction on patient-reported outcome measures after transposition osteotomy of the acetabulum (TOA), a spherical periacetabular osteotomy.Methods:We retrospectively reviewed 442 patients (582 hips) with hip dysplasia who underwent TOA between 1998 and 2019 and completed validated questionnaires, including the visual analog scale (VAS) for pain and satisfaction and the Hip disability and Osteoarthritis Outcome Score (HOOS). The median follow-up was 12 years. Associations between patient-reported outcome measures and preoperative variables and postoperative acetabular coverage (lateral center-edge angle, anterior wall index, and posterior wall index) were analyzed.Results:Older age was negatively correlated with HOOS-ADL (r = −0.26, P < 0.001) and HOOS-sports/recreation (r = −0.25, P < 0.001). Male patients reported lower median HOOS-QOL than female patients (P = 0.038). Patients with Tönnis grade 0 had higher median satisfaction-VAS than those with grade 2 (P = 0.031), and higher median HOOS-ADL, sports/recreation, and QOL subscales than those with grade 1 or 2. For postoperative anterior wall index, the deficient group had higher VAS-pain (P = 0.045) and lower HOOS-pain (P = 0.047) than the normal group. For postoperative posterior wall index, the excessive group had lower HOOS-pain than the normal group (P = 0.029).Conclusion:Even in preserved hips after TOA, sagittal plane acetabular correction influenced postoperative pain, whereas age, sex, and Tönnis grade affected satisfaction, functional capacity, and QOL. These insights have implications for refining surgical indications and acetabular reorientation strategies, improving postoperative patient experience.

This paper proposes a low-code development framework for Internet of Things (IoT) applications, integrating a visual data flow programming interface with the lightweight scripting language–mruby. The aim is to reduce the complexity and technical barriers traditionally associated with embedded programming, particularly in environments with resource-constrained microcontrollers.The system enables users to design application logic visually with Node-RED, a popular data-flow implementation tool. The generated data flow is exported as a JSON file, which is then parsed by a custom mruby code generator. This generator translates the data flow into executable Ruby code, then compiles it into compact bytecode using the compiler. The resulting bytecode is then deployed to microcontrollers running a minimal mruby virtual machine (VM), enabling the efficient execution of application logic without the need for a full interpreter or operating system. To validate the system, a prototype was implemented and evaluated on an RBoard — a development board based on a PIC microcontroller with limited memory and computing resources. A simple IoT application was designed to read temperature sensor data and control an LED based on a threshold. The experimental results confirmed that the system could handle sensor input, control logic and hardware-level output in real time using only the automatically generated code.This framework significantly reduces development time and programming effort, making embedded development accessible to non-experts and facilitating rapid prototyping. Combining visual programming with mruby bytecode execution ensures ease of use and runtime efficiency. Future work will focus on extending node types, enhancing debugging and simulation capabilities, facilitating wireless deployment and expanding support for a wider range of microcontrollers. This approach demonstrates a practical path towards scalable, maintainable and user-friendly IoT development.

This study assessed the effects of astaxanthin supplementation on chronic and acute digital eye strain in school-aged children (10-14years) and evaluated its safety. While previous studies focused on adults, this study examined astaxanthin's effects on developing eyes. A randomized, double-blind, placebo-controlled trial was conducted over 84days involving 64 children engaged in≥4h of screen time daily and experiencing mild to moderate computer vision syndrome (CVS) symptoms as indicated by a CVS-Questionnaire (CVS-Q) score≥8 and<19. Participants received a daily 4-mg astaxanthin soft capsule for 84days. Primary outcomes were measured using CVS-Q, while secondary outcomes included visual fatigue Likert scale (VFLS), visual acuity, spherical equivalence, near point of accommodation, near exophoria, dry eye intensity, pupil size, stereopsis, blinking frequency, immunity, and safety variables. Of the 64 participants (mean age 11.5-11.7years), 35 were male and 29 were female. Astaxanthin supplementation significantly improved CVS-Q scores after 84days (-4.00±4.05 arbitrary units (A.U.) from baseline, p<0.0001) compared to placebo (-1.72±3.61 A.U., p<0.05), a 20% between group difference. The mean VFLS scores were significantly lower in the astaxanthin group (11.55±5.78 A.U.) compared to placebo (15.78±7.12 A.U., p=0.01), showing a 27% improvement after 84days. Stereopsis improved significantly after acute visual load at 28 and 84days (p<0.05, p<0.0001 vs. placebo, respectively), and pupillary light reflex improved after 84days (p<0.05 vs. placebo). Tear production increased after 14, 56, and 84days (p<0.05, p<0.001, and p<0.001 vs. baseline, respectively) in the astaxanthin group, with no significant intergroup difference in the Schirmer I test, visual acuity, spherical equivalence, near point of accommodation, near exphoria, immune markers, or safety variables. Astaxanthin supplementation effectively reduced chronic and acute digital eye strain, while enhancing objective measures of visual performance in school-aged children, underscoring thebenefits of astaxanthin in pediatric visual health and performance. NIH ClinicalTrials.gov (Identifier: NCT05602402); Clinical Trials Registry India (Registration Number: CTRI/2022/10/046606).

Lipoic acid trisulfide, a sulfane sulfur-containing trisulfide of α-lipoic acid, holds promise in pharmaceuticals, yet knowledge gaps persist regarding its synthesis, properties, and stability. Here, we synthesized the lipoic acid trisulfide with a purity exceeding 99% from α-lipoic acid on a gram scale and obtained novel β-cyclodextrin clathrates (84%-95% yield). Differential scanning calorimetry confirmed the inclusion of lipoic acid trisulfide in β-cyclodextrins. The resulting β-cyclodextrin clathrates exhibited significant improvements in water solubility and thermal stability. This pioneering study demonstrated a novel approach to the practical preparation of trisulfide and its β-cyclodextrin clathrates as active ingredients, paving the way for clinical development.

薬液注入工法は，止水や強度増加を目的とした地盤改良工法の一つであり，軟弱地盤対策には欠かせないものである。これまで多くの施工実績を有する薬液注入工法であるが，工法の性質上，改良範囲や改良強度が不均一になることが危惧されている。本研究では，薬液の浸透挙動に影響を与える原因を3つ挙げ，それぞれの項目に対し影響評価を行った。1つ目は，薬液の種類によって異なる粘性と地盤の透水性が薬液の浸透挙動に与える影響を，浸透流解析によって評価した。2つ目は，地盤の浸透不確実性が薬液の浸透挙動に与える影響を，浸透流解析とモンテカルロ・シミュレーションによって評価した。3つ目は，薬液のレオロジー特性が浸透挙動に与える影響を，MPS-DEM連成解析によって評価した。これら3つの項目の評価の流れを示すことで，薬液注入工法における新たな性能評価手法の提案を目的としている。

Effects of size and crystallinity of a quadruple perovskite oxide, CaCu3Fe4O12, were investigated for its catalytic activity for the oxygen evolution reaction (OER). Pristine CaCu3Fe4O12 powder sample was synthesized under high-pressure and high-temperature conditions of 8 GPa and 1000°C, and a portion was treated by ball milling for 120 min to obtain a powder sample with smaller particle size. The specific surface area significantly increased from 0.38 to 10.30 m2g−1 by ball-milling, leading to increased OER activity. However, it was found that the milling did not improve the OER activity efficiency in proportion to that expected from the increase in specific surface area as determined by Brunauer-Emmett-Teller analysis of adsorption/desorption isotherms measured with nitrogen gas because the crystallinity was lowered by ball milling, which suppressed the catalytic activity. This study provides important information on how to achieve the best OER catalytic performance in terms of both size and crystallinity.

Background and Objective: Turfgrass resistance to heavy traffic and wear damage is one important quality in turfgrass. Since it differs within species, some wear resistance tests have been developed to further differentiate turfgrasses but they are more laborious and require longer time. Therefore, the aim of the study was to build an efficient tread loading system and evaluate its load condition on 3 commercial turfgrass cultivars: Zoysia matrella Emerald, Zoysia japonica Meyer, Cynodon dactylonCynodon transvaalensis Tifway and a new Zoysia matrella cultivar Wakaba. Materials and Methods: A multiple tread loading system was constructed to accommodate 32 grass trays. Treading test was conducted on 4 turfgrass cultivars and the number of erect stems, stolon dry weight and green turf coverage were analyzed. Results: The newly registered cultivar Wakaba had the highest number of erect stems and green coverage in both treading and non-treading (control) tests as compared to zoysiagrasses Emerald and Meyer, while bermudagrass Tifway least performed in all tests. Conclusion: It is concluded that tread loading system is efficient to analyze treading damage for multiple turfgrasses in a short period of time. In addition, the new cultivar Zoysia matrella Wakaba has high resistance to treading and utilization of this cultivar is recommended.

Artificial spherical sands were cured using water glass as a binder with or without addition of porous silica to prepare the test piece and aluminum alloy casting core. In order to clarify the curing and collapsibility mechanism of inorganic sand mold, the cross-linked structure between their particles were evaluated by SEM observation. A three-dimensional network of crosslinking bridges derived from water glass formed between the spherical particles enables the preparation of a core with sufficient strength for casting. The water glass added to cure the core requires less than 2 wt% by weight for the sand prepared by the melting method and about a third as much as that prepared by the sintering method. The high collapsibility of such an inorganic mold is due to the rapid elongation of crosslinking bridges between the particles when heated above a certain temperature so that the particles are separated from each other. Especially for spherical particles with a smooth surface, the relatively small amount of water glass for curing would cause collapsibility accelerated by the thinning of the crosslinked body wall occurring simultaneously with elongation. Furthermore, the addition of porous silica would induce elongation at a lower temperature as compared to when porous silica is not added, and is extremely effective for improving the collapsibility of the inorganic sand mold.