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Nursing students experience higher levels of stress and more sleep-related problems than other students; however, the relationship of chronotype to nursing students' sleep status and health-related quality of life (HRQOL) is unclear. This cross-sectional, observational study investigated whether chronotype affected Japanese nursing college students' sleep and HRQOL. Nursing students completed the Attribute Questionnaire about Subject Background, Japanese Version Morningness‒Eveningness Questionnaire (MEQ), Munich Chrono-Type Questionnaire‒Japanese Version (MCTQ), Japanese Version of the Pittsburgh Sleep Quality Index (PSQI), SF-12v2 Standard, Japanese Version 2.0 (SF-12), Japanese Translation of Profile of Mood States 2nd Edition‒Adult Short (POMS2). Of the 241 students (mean age 20.16 ± 1.80 years; 80.9% female), 80 (33.2%) had evening, 142 (58.9%) had intermediate, and 19 (7.9%) had morning chronotype. The overall total PSQI score was 6.86 ± 2.97. Additionally, 141 students (64.1%) scored ≥ 6, suggesting disturbed sleep. Approximately 80% of the evening chronotype students had a total PSQI score of 8.34 ± 3.11, clearly indicating disturbed sleep. Sleep-related parameters (total PSQI score, bedtime, sleep latency, wake-up time, sleep duration, social jetlag) were worse in evening than in other chronotypes. SF-12 and POMS2 did not differ among chronotypes. Thus, evening chronotype nursing students require sleep-related support from early on.

Osteotomy of the distal fibula or anterolateral corner of the tibia is usually required to fix a displaced osteochondral fracture of the talus that is located central to posterior area of the lateral talar dome. However, osteotomy is an invasive procedure and is associated with complications, including nonunion, persistent pain, and hardware-related problems. Lateral inverted osteochondral fracture of the talus (LIFT) lesion is an extremely rare type of displaced osteochondral lesion of the talus. We describe a case in which a LIFT lesion was fixed using an innovative surgical approach, inverting capsulo-lateral fibulotalocalcaneal ligament (LFTCL)-fibular periosteum complex, with a favorable short-term clinical outcome.

This study was conducted to present remnant-preserving anterior cruciate ligament (ACL) augmentation as a useful option for partial ACL injury in multiligament knee injury (MLKI) cases, which may also contribute to conserving graft resources. The present study involved patients diagnosed with MLKI at our institute from Spring 2006 to February 2021. A total of 71 MLKI cases were provided surgery due to knee instability and disability. For every patient, an arthroscopic diagnostic was performed to ensure that ACL tear and a remnant were present. When the ACL remnant was classified into group 2, 3, or 4 of Nakamae's classification, remnant-preserved single bundle ACL augmentation was performed. Graft selection and the combination of injured ligaments were evaluated. The side-to-side difference under an anterior tibial load of 134 N with an arthrometer and the leg symmetry index at 60 degrees/s were measured. The present procedure was performed for five cases (male/female: 4/1, mean age: 33.6 years). The mean follow-up period was 26.4 months. The combination of torn ligaments was as follows: 3 cases of ACL + medial collateral ligament, one case of ACL + posterior cruciate ligament, and one case of ACL + posterolateral corner. An ACL augmentation graft was performed using an ipsilateral gracilis tendon in 2 cases, a contralateral full semitendinosus tendon in 2 cases, and the ipsilateral distal 1/2 of the semitendinosus tendon in 1 case. The mean side-to-side difference was 1.07 ± 0.4 mm. The mean leg symmetry index was 82.6 ± 12.2% in knee extension and 96.3 ± 9.9% in knee flexion. Although the present study was a small case series, the remnant-preserved single-bundle ACL augmentation for MLKI surgery provided good clinical outcome and conserved the graft resource. Even in the MLKI case, this technique is one of the useful surgical options. The level of evidence of this study is level IV (case series).

For anterior cruciate ligament (ACL)-deficient patients, using a single bone-patellar tendon-bone (BPTB) graft for the double-bundle concept is one of the suitable approaches for acquiring better stability and reducing bone tunnel enlargement compared with the use of hamstring grafts. At least 10-mm width of BPTB autograft is needed to achieve this concept; however, it is larger than one-third of the patellar tendon width for small or middle physique patients. This study aimed to assess the clinical and radiographic outcomes of BPTB and gracilis (G) composite autografts for primary double-bundle ACL reconstruction in Asian athletes. Thirty-two Asian patients undergoing double-bundle ACL reconstruction with 7.0 to 7.5 mm of BPTB and 5.0 to 5.5 mm of G composite grafts were compared with 43 double-bundle ACL reconstruction with hamstring graft cases. The BPTB graft was used for the anteromedial bundle (AMB), with the G graft for the posterolateral bundle (PLB). Percentage of femoral bone tunnel enlargement compared with the original size was determined by computed digital radiographs on the first postoperative day and at 12 months in the anteroposterior (AP) and lateral views. Standard clinical evaluations, including the limb symmetry index (LSI), were also performed. Less PLB tunnel enlargement was found in the BPTB + G group than in the hamstring group in the AP (101.9 ± 22.9 vs.113.7 ± 20.6%, p = 0.031) and lateral views (104.4 ± 18.1 vs. 120.6 ± 23.4%, p

BackgroundKnee extensor structure disruption is sometimes combined with multi-ligament knee injury (MLKI). These cases could not be classified into the previous classification for knee dislocation or MLKI. To propose a new classification of MLKI that addresses both femorotibial and patellofemoral (PF) factors.MethodsThe present study involved patients diagnosed with MLKI at our institute. Cases with two or more injured structures diagnosed clinically and by MRI and X-ray examinations were included. Details of injured structures were defined as follows: ‘cruciate ligaments’, including the ACL and PCL; ‘collateral ligaments’, including the MCL and the posterolateral corner (PLC); and the ‘PF joint factor’, including the medial patellofemoral ligament (MPFL), quadriceps tendon, and patellar tendon. A total of 65 cases met the inclusion criteria from 2007 to August 2020 and were enrolled in this study.Based on the number of injured structures, cases were categorized as: Type A, two structures injured; Type B, three structures injured; Type C, four structures injured; and Type D, five structures injured. Depending on the combination of injured structures, they were subdivided into 1 to 5 in Types A and B and into 1 to 3 in Type C. Additional injuries were subdivided as follows: MLKI with fracture was defined as X, with neurovascular injury as Y, and both fracture and neurovascular injury as Z. MLKI cases were divided into both Schenck’s KD classification and the present classification.ResultsFourteen of 65 cases (21.5%) could not be categorized using Schenck’s KD classification; two cases of PLC+MPFL (Type-A5 in new classification), ACL+PLC with periarticular fracture (Type-A1-X), and single cases of ACL+MCL+PLC (Type-B2), ACL+PCL+MCL+PLC+MPFL (Type-D), ACL+MPFL (Type-A4), ACL+MCL+MPFL (Type-B3), PCL+PLC+ patellar tendon with periarticular fracture (Type-B3-X), and PCL+ patellar tendon (Type-A4), ACL+PLC with neurovascular injury (Type-A1-Y), and three cases of PCL+PLC with complications (Type-A1-X, -Y, -Z). With the new classification for MLKI and complications, all cases were successfully assigned to each category.ConclusionIn the present classification, every combination of MLKI cases containing both tibiofemoral and patellofemoral factors, with or without complications, was successfully classified into a suitable category.

The present study aimed to assess the appropriate oxygen saturation target in patients with pediatric respiratory diseases by lowering the oxygen saturation target from SpOThe present, prospective, single-arm intervention trial enrolled pediatric inpatients with bronchiolitis, bronchitis, pneumonia, and asthma. The oxygen saturation target was lowered from SpOIn total, 248 patients completed the study. Patients with bronchiolitis, bronchitis, pneumonia, and asthma had an interval between the two cut-off points of 23.9, 15.5, 19.1, and 13.8 h, respectively, (mean 17.2 h; 95% confidence interval 15.0-19.5).In generally healthy children, setting the oxygen saturation target at SpO

Background Acute lower respiratory infection (ALRI) remains the leading cause of death in children worldwide, and viruses have been the major causative factors of ALRI after the introduction of bacterial conjugate vaccines. In Myanmar, ALRI is associated with high morbidity and mortality in children. However, detailed information on ALRI is currently lacking. Methods We conducted a prospective study to investigate the viral aetiologies, clinical manifestations, and outcomes of ALRI in hospitalised children at the Yankin Children Hospital, Yangon, Myanmar from May 2017 to April 2019. The World Health Organization’s definitions of ALRI and severe ALRI were used with minor modifications. For the patients with suspected viral ALRI, a nasopharyngeal swab was obtained, and rapid tests for influenza and respiratory syncytial virus (RSV) were performed, followed by real-time PCR for the 16 respiratory viruses causing ALRI. Clinical information was extracted from the medical records. Results Among the 5463 patients admitted with a diagnosis of ALRI, 570 (10.4%) were randomly enrolled in the study. The median age of the patients was 8 months (interquartile range, 4–15 months). The most common symptoms were cough (93%) and difficulty of breathing (73%), while the most common signs were tachypnoea (78%) and chest indrawing (67%). Sixteen potentially causative viruses were detected in 502 (88%) patients, with RSV B (36%) and rhinovirus (28%) being the most commonly detected. Multiple viruses were detected simultaneously in 221 patients (37%). Severe ALRI was diagnosed in 107 patients (19%). The mortality rate was 5%; influenza virus A (29%) and RSV B (21%) were commonly detected in such cases. Conclusions Viral ALRI in children has significant morbidity and mortality rates in Myanmar. RSV and rhinovirus were the most commonly detected, while influenza virus and RSV were the most common causes of mortality.

Background Acute lower respiratory infection (ALRI) remains the leading cause of death in children worldwide, and viruses have been the major cause of ALRI. In Myanmar, ALRI is associated with high morbidity and mortality in children, and detailed information on ALRI is currently lacking. Methods This prospective study investigated the viral aetiologies, clinical manifestations, and outcomes of ALRI in hospitalised children aged 1 month to 12 years at the Yankin Children Hospital, Yangon, Myanmar from May 2017 to April 2019. The sample size was set to 300 patients for each year. Two nasopharyngeal swabs were obtained for the patients with suspected viral ALRI; one for rapid tests for influenza and respiratory syncytial virus (RSV), and the other for real-time PCR for the 16 ALRI-causing viruses. Pneumococcal colonization rates were also investigated using real-time PCR. Clinical information was extracted from the medical records, and enrolled patients were categorised by age and severity for comparison. Results Among the 5463 patients admitted with a diagnosis of ALRI, 570 (10.4%) were enrolled in this study. The median age of the patients was 8 months (interquartile range, 4–15 months). The most common symptoms were cough (93%) and difficulty in breathing (73%), while the most common signs of ALRI were tachypnoea (78%) and chest indrawing (67%). A total of 16 viruses were detected in 502 of 570 patients’ samples (88%), with RSV B (36%) and rhinovirus (28%) being the most commonly detected. Multiple viruses were detected in 221 of 570 samples (37%) collected from 570 patients. Severe ALRI was diagnosed in 107 of 570 patients (19%), and RSV B and human rhinovirus were commonly detected. The mortality rate was 5%; influenza virus A (29%) and RSV B (21%) were commonly detected, and stunting and lack of immunization were frequently observed in such cases. Additionally, 45% (259/570) of the patients had pneumococcal colonization. Conclusions Viral ALRI in hospitalised children with a median of 8 months has significant morbidity and mortality rates in Myanmar. RSV and rhinovirus were the most commonly detected from nasopharyngeal swabs, while influenza virus and RSV were the most frequently associated with fatal cases.

ObjectivesMedical examinations for adult elite athletes are performed all over the world, however, no studies in the relevant English literature have reported on orthopaedic medical examinations for young amateur athletes. The purpose of this study was to report the results of orthopaedic medical examinations of the spine and lower extremities in young amateur athletes.MethodsThis repeated cross-sectional study from 2014 to 2018 included a total of 323 young amateur athletes (age, 12–18 years) who were active in one of the following four sports: boxing, canoeing, weightlifting and track and field. The orthopaedic medical examination consisted of six assessments (physical examinations, the generalised joint laxity, muscle and joint tightness, static alignment and muscle volume of the lower extremities and the medial longitudinal arch of the foot). Questions regarding pain in the spine and lower extremities were also performed.ResultsAmong 323 young amateur athletes, 17 (5.3%) had received orthopaedic treatment at the time of the medical examination, with spondylolysis being the most common cause (29.4%, 5/17). Among 306 young athletes who had not received orthopaedic treatment, 61 (19.9%) had at least one positive finding in physical examinations or had pain in the spine or lower extremities. Anterior drawer test of the ankle and Kemp test for the spine accounted for 34% and 28% of positive findings, respectively. Low back pain and knee pain accounted for 58% and 16% of pain, respectively.ConclusionsThe present study showed that approximately one-fifth of young amateur athletes who had not received orthopaedic treatment had pain in the spine and lower extremities and positive findings in physical examinations that may require orthopaedic treatments. In addition to the early detection of injuries, orthopaedic medical examinations for young amateur athletes provide an opportunity to educate such athletes.

Objective: This study examines the job satisfaction of Mongolian hospital nurses by comparing their status and workload of Mongolian nurses with Japanese nurses’ one. Settings and participants/Methods: Survey data were collected from randomly selected 200 nurses (100 were Mongolians and the other 100 were Japanese) who agreed to participate in the survey. Data were collected through a self-administered survey questionnaire. Survey items were age, the duration of work experience, work position, health condition, accumulated fatigue, stress level, and whether having family members who need child care or nursing care. Collected data were analyzed by t-test and Wilcoxon Rank Sum test. Results: The average age of Mongolian nurses was significantly lower than that of Japanese nurses. Consequently, the average work experience of Mongolian nurses was less than that of Japanese nurses. More Japanese than Mongolian nurses had family members in need of care. Job satisfaction and status were significantly higher among Japanese than Mongolian nurses. However, Japanese nurses have family members who need child care or nursing care at a higher rate than Mongolian nurses. Job satisfaction of Japanese nurses about their work and job status was significantly higher than Mongolian nurses’ one. However, the opposite result was found in the job satisfaction about their workload. The influence of the relationships among nurses on the job satisfaction was significantly greater in Mongolian nurses than in Japanese nurses. Job satisfaction of Japanese nurses about their salaries was significantly higher than Mongolian nurses’ one. Conclusion: In order to raise nurses’ job satisfaction in Mongolia, it is necessary to raise their “occupational status” and salary of nurses.

Since mid-February, 2020, coronavirus disease-2019 (COVID-19) has been spreading in Cambodia and, as of April 9, 2020, the Ministry of Health has identified 119 polymerase chain reaction (PCR)-positive cases. However, the PCR test is available in only two specialized institutes in the capital city Phnom Penh; therefore, exact and adequate identification of the cases remains still limited. Many vulnerable newborn infants have been admitted to the neonatal care unit (NCU) at the National Maternal and Child Health Center in Phnom Penh. Although the staff have implemented strict infection prevention and control measures, formidable gaps in neonatal care between Cambodia and Japan exist. Due to the shortages in professional workforce, one family member of sick newborn(s) should stay for 24 hours in the NCU to care for the baby. This situation, however, may lead to several errors, including hospital-acquired infection. It is crucial not only to make all efforts to prevent infections but also to strengthen the professional healthcare workforce instead of relying on task sharing with family members.

Despite numerous genetic studies on bone metabolism, understanding of the specific mechanisms is lacking. We developed an efficient screening system to identify novel genes involved in bone metabolism using mutant mouse strains registered with the Exchangeable Gene Trap Clones (EGTC) database. From 1278 trap clones in the EGTC database, 52 candidate lines were selected in the first screening, determined based on “EST profile”, “X-gal”, “Related article”, and “Novel gene”. For the second screening, bone morphometric analysis, biomechanical strength analysis, bone X-gal staining, etc. were performed on candidate lines. Forty-two male trap lines (80.8%) showed abnormalities with either bone morphometric analysis or biomechanical strength analysis. In the screening process, X-gal staining was significantly efficient (P = 0.0057). As examples, Lbr and Nedd4 trap lines selected using the screening system showed significant bone decrease and fragility, suggesting a relationship with osteoblast differentiation. This screening system using EGTC mouse lines is extremely efficient for identifying novel genes involved in bone metabolism. The gene trap lines identified as abnormal using this screening approach are highly likely to trap important genes for bone metabolism. These selected trap mice will be valuable for use as novel bio-resources in bone research.

Objectives To clarify the frequency of musculoskeletal problems in public elementary and junior high school children and to determine the advantages and problems of musculoskeletal examinations. Study design School-based cross-sectional study nested in a cohort. Methods We examined 41,376 public elementary and junior high school children (aged 6–15 years) in Miyazaki, Japan, from 2008 to 2014. Participation was voluntary. Participants received an in-school primary musculoskeletal examination (clinical examination with check items and a questionnaire) and a secondary examination at an orthopaedic outpatient clinic as indicated. Estimated prevalence rates for musculoskeletal problems were calculated from the results of both examinations. Results The total estimated prevalence of musculoskeletal problems was 8.6%. Prevalence by school grade ranged from 3.2% to 13.7%. Estimated prevalence rates increased as grade increased and were higher in junior high school students than in elementary school students. The secondary examination identified musculoskeletal problems on the back (65.4%), knee (8.1%), ankle or feet (7.3%) and elbow (5.4%). Of those referred for a secondary examination, 44.4% had not reported musculoskeletal complaints on the initial questionnaire. Overall, 69.8% of problems diagnosed in the secondary examination were previously undiagnosed. Conclusions School-based musculoskeletal examination enables early detection of abnormal growth and disorders of the locomotive organs and is expected to support children's musculoskeletal growth and development. We recommend musculoskeletal examinations as part of school check-ups in Japan. Our findings suggest musculoskeletal examinations should be conducted for students in higher elementary school grades and for all junior high school students. Evaluation should include both direct clinical examination and questionnaires.

In order to clarify the role of the 1-substituent of quinazoline derivatives in their inhibitory activity against poly(ADP-ribose) polymerase (PARP), two novel inhibitors, 1 [8-hydroxy-1-(3-morpholinopropyl)-quinazoline-2,4(1H,3H)-dione] and 2 [8-hydroxy-1-(3-phenoxypropyl)-quinazoline-2,4(1H,3H)-dione], were synthesized and subjected to X-ray crystal analysis in complex with the PARP C-terminal catalytic domain (PARP-CD), which requires NAD+ coenzyme for biological function. The nicotinamide-mimicking part of the quinazoline skeleton of 1 and 2 were both located at the nicotinamide subsite of the NAD+-binding pocket in the same manner as previously reported inhibitors: three hydrogen bonds [(Gly-863)NH-O12, (Gly-863)O-HN3 and (Ser-904)O(gamma)-O12] and stacking interaction between the Tyr-907 phenol and the quinazoline ring. On the other hand, the N-morpholinoprop-3-yl moiety introduced at the 1-position of the quinazoline ring in 1 bridged the large gap between the donor site and the acceptor site through a (Met-890)NH-O20(morpholine) hydrogen bond, where the donor and the acceptor sites are classified as the binding sites of NAD+ and the ADP moiety of the poly(ADP-ribose) chain, respectively. In contrast, the N-phenoxyprop-3-yl moiety in 2 formed hydrophobic interactions close to the adenosine-binding site of NAD+, unlike the hydrogen bond such as in 1. As the inhibitory activities of 1 and 2 for PARP were much more potent than those of the unsubstituted nicotinamide analogues, these results suggest that the occupation of the proximal region of the ADP phosphate-and adenosine-binding subsite of the donor site or that of the gap between the donor and the acceptor site by the 1-substituent of quinazoline may increase the inhibitory activity considerably. The nearly equal inhibitory activities of 1 and 2, despite of their different binding modes at the active site, indicate that this 1-substituent is promising in improving the bioavailability of the inhibitor without compromising its inhibitory activity.

Effects of a new calcium antagonist, CD-832, on intracranial pressure (ICP), vertebral blood flow (VBF) and common carotid blood flow (CCBF) were investigated in dogs and the results were compared with findings for nifedipine and diltiaem. Dogs were anesthetized with sodium pentobarbital and a 20-gauge needle was inserted into the cisterna magna for ICP determination. Mean arterial blood pressure (MBP), heart rate (HR), CP, VBF and CCBF were measured before and during the continuous intravenous infusion of CD-832 (0.3, 1 and 3 microg/kg/min), nifedipine (0.1, 0.3 and 1 microg/kg/min) or diltiazem (1, 3 and 10 microg/kg/min). Although the three drugs caused a comparable hypotension, differences were evident in effects of these agents on ICP, VBF and CCBF. Nifedipine and diltiazem but not CD-832 significantly increased ICP, VBF and CCBF. These results suggest that CD-832 is a unique calcium antagonist which does not increase ICP during hypotension. Because the most evident side effects of calcium antagonists are caused by vasodilation and include headache and flushing, CD-832 may possibly be useful to treat subjects with hypertension or angina pectoris.

(4 R )-(−)-2-(Nicotinoylamino)ethyl 3-nitrooxypropyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylate ( 1 ), a new calcium antagonist, was synthesized via both enantioselective hydrolysis and transesterification of prochiral bis[2-(nicotinoylamino)ethyl]ester · 2HCl ( 5 ) by using enzymes. Hydrolysis of 5 by proteases originated from Aspergillus melleus and Bacillus licheniformis etc. in aqueous media afforded (4 R )-(−)-3-[2-(nicotinoylamino)-ethoxycarbonyl]-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-5-carboxylic acid ( 6 ) in more than 99% e.e., which was converted to 1 by esterification with 3-nitrooxypropyl bromide. Enzymatic transesterification of 5 with 3-nitrooxypropanol gave 1 in more than 99.5% e.e. directly.

(4 R )-(−)-2-(Nicotinoylamino)ethyl 3-nitrooxypropyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylate ( 1 ), a new calcium antagonist, was synthesized via both enantioselective hydrolysis and transesterification of prochiral bis[2-(nicotinoylamino)ethyl]ester · 2HCl ( 5 ) by using enzymes. Hydrolysis of 5 by proteases originated from Aspergillus melleus and Bacillus licheniformis etc. in aqueous media afforded (4 R )-(−)-3-[2-(nicotinoylamino)-ethoxycarbonyl]-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-5-carboxylic acid ( 6 ) in more than 99% e.e., which was converted to 1 by esterification with 3-nitrooxypropyl bromide. Enzymatic transesterification of 5 with 3-nitrooxypropanol gave 1 in more than 99.5% e.e. directly.

Epoxyeicosatrienoic acids (EETs) are the major arachidonic acid products of cytochrome P-450 epoxygenase and further metabolized by soluble epoxide hydrolase (sEH) to their corresponding dihydroxye...

Activation of the Na+/Ca2+ exchanger may contribute to Ca2+ overload during reperfusion after transient ischemia. We examined the effects of 2-[4-[(2,5-difluorophenyl) methoxy]phenoxy]-5-ethoxyaniline (SEA0400), a selective inhibitor of Na+/Ca2+ exchange, on a canine model of ischemia/reperfusion injury (myocardial stunning). Myocardial stunning was induced by a 15-min occlusion of the left anterior descending coronary artery followed by a 4-h reperfusion in anesthetized open-chest dogs. Reperfusion gradually restored myocardial percent segment shortening but remained depressed during a 4-h reperfusion period. A bolus intravenous injection of SEA0400 (0.3 or 1.0 mg/kg), given 1 min before reperfusion, improved significantly the recovery of percent segment shortening in the ischemic/reperfused myocardium. SEA0400 did not affect the hemodynamics and electrocardiogram parameters. In addition, SEA0400 did not affect reperfusion-induced change in coronary blood flow. These results suggest that the Na+/Ca2+ exchanger is involved in the stunned myocardium of dogs after reperfusion, and that SEA0400 has a protective effect against myocardial stunning in dogs.

The concept of drug-likeness, an important characteristic for any compound in a screening library, is nevertheless difficult to pin down. Based on our belief that this concept is implicit within the collective experience of working chemists, we devised a data set to capture an intuitive human understanding of both this characteristic and ease of synthesis, a second key characteristic. Five chemists assigned a pair of scores to each of 3980 diverse compounds, with the component scores of each pair corresponding to drug-likeness and ease of synthesis, respectively. Using this data set, we devised binary classifiers with an artificial neural network and a support vector machine. These models were found to efficiently eliminate compounds that are not drug-like and/or hard-to-synthesize derivatives, demonstrating the suitability of these models for use as compound acquisition filters.

The Na(+)/Ca(2+) exchanger (NCX) is involved in myocardial ischemia-reperfusion injuries. We examined the effects of 2-[4-[(2,5-difluorophenyl)methoxy]phenoxy]-5-ethoxyaniline (SEA0400), a potent and selective inhibitor of NCX, on myocardial ischemia-reperfusion injury models. In canine cardiac sarcolemmal vesicles and rat cardiomyocytes, SEA0400 potently inhibited the Na(+)-dependent 45Ca(2+) uptake with an IC(50) value of 90 and 92 nM, compared with 2-[2-[4-(4-nitrobenzyloxy)phenyl]isothiourea (KB-R7943, 7.0 and 9.5 microM), respectively. In rat cardiomyocytes, SEA0400 (1 and 3 microM) attenuated the Ca(2+) paradox-induced cell death. In isolated rat Langendorff hearts, SEA0400 (0.3 and 1 microM) improved the cardiac dysfunction induced by low-pressure perfusion followed by normal perfusion. In anesthetized rats, SEA0400 (0.3 and 1 mg/kg, i.v.) reduced the incidence of ventricular fibrillation and mortality induced by occlusion of the left anterior descending coronary artery followed by reperfusion. These results suggest that SEA0400 is a most potent NCX inhibitor in the heart and that it has protective effects against myocardial ischemia-reperfusion injuries.

Ortho-alkylation par l'intermediaire d'une transposition sigmatrope [2+3]; les isopropylthio-1' alkyl-2' phenols obtenus peuvent se cycliser: on prepare de cette facon la coumarine, le chromanne, le dimethyl-2,2 chromene et l'α-tocopherol

2-[4-(3-Methyl-2-butenyl)phenyl]propionic acid was synthesized in 82% yield via nickel(II) chloride or dichlorobis[η5-cyclopentadienyl]titanium-catalyzed hydromagnesation of 1-(3-methyl-2-butenyl)-4-vinylbenzene obtained in ca. 63–68% yield by the coupling reaction of 4-(3-methyl-2-butenyl)phenylmagnesium chloride with vinyl chloride.

Synthese d'acides alcene-1″(-2″)yl-4' phenyl-2 propioniques. Activites antiinflammatoire et analgesique de ces composes et comparaison avec celles de l'ibuprofene

The 4-alkenylchlorobenzenes (I), prepared from p-chlorobenzene or 4-chloromethylchlorobenzene by normal alkylation reactions with organometallic compounds, undergo Grignard reaction with (II), yielding the title compounds (III).

2-[4-(3-Methyl-2-butenyl)phenyl]propionic acid was synthesized in 82% yield via nickel(II) chloride or dichlorobis[η5-cyclopentadienyl]titanium-catalyzed hydromagnesation of 1-(3-methyl-2-butenyl)-4-vinylbenzene obtained in ca. 63–68% yield by the coupling reaction of 4-(3-methyl-2-butenyl)phenylmagnesium chloride with vinyl chloride.

ortho-Alkylphenols have been prepared from phenol and dialkyl sulphoxides via[2,3]sigmatropic rearrangement, using thionyl chloride or phenyl chlorosulphinate as an activator of sulphoxides. In the same manner, ortho-phenylthiomethylphenol has been prepared in good yield. When ethyl phenyl sulphoxide, diallyl sulphoxide, and methyl methylsulphinylacetate were used as sulphoxides, none of the expected products were obtained. Salicylaldehyde has been prepared in moderate yield, when methyl methylthiomethyl sulphoxide was used as a sulphoxide. 3-(2-Hydroxyphenyl)propionic acid derivatives, which were obtained from substituted phenols and dimethyl 3,3′-sulphinyldipropionate, have been cyclized to give the corresponding coumarins in good yields.