Psychiatry Investig
July 2024
Objective: This study was performed to evaluate the efficacy and safety of lurasidone (160 mg/day) compared to quetiapine XR (QXR; 600 mg/day) in the treatment of acutely psychotic patients with schizophrenia.
Methods: Patients were randomly assigned to 6 weeks of double-blind treatment with lurasidone 160 mg/day (n=105) or QXR 600 mg/day (n=105). Primary efficacy measure was the change from baseline to week 6 in Positive and Negative Syndrome Scale (PANSS) total score and Clinical Global Impressions severity (CGI-S) score.
A highly efficient asymmetric [3+2] and [4+2]-annulation of cyclic -sulfonyl ketimines with γ- or δ-hydroxy-α,β-unsaturated ketones has been developed. This innovative reaction employs an organocatalytic approach, utilizing a hydrogen-bonding bifunctional squaramide-based catalyst. The process enables precise synthesis of chiral polyheterotricyclic oxazolidines and 1,3-oxazinane derivatives, revealing intricate structures with incorporated chiral quaternary centers.
View Article and Find Full Text PDFThe 1,4-benzodiazepine structural framework is a fascinating element commonly found in biologically active and pharmaceutically relevant compounds. A highly efficient method for synthesizing 1,4-benzodiazepin-3-ones is described, involving a [4+3]-cycloaddition reaction between 2-amino-β-nitrostyrenes and α-bromohydroxamate, with CsCO used as a base. This process yielded the desired 1,4-benzodiazepines in good yields.
View Article and Find Full Text PDFA highly efficient enantioselective [4 + 2] cycloaddition of 2-amino-β-nitrostyrenes with cyclic -sulfonyl ketimines has been developed. This reaction utilizes an organocatalytic approach, employing a multiple-hydrogen-bonding bifunctional squaramide-based catalyst. The process allows for the precise synthesis of chiral polycyclic benzosultams, showcasing intricate structures that incorporate chiral quaternary centers.
View Article and Find Full Text PDFA novel method for the enantioselective synthesis of spiro -heterocyclic oxindoles has been developed, employing asymmetric [4 + 2]-cycloadditions of 2-aminophenyl enones with isatin-derived ketimines. This method employs an organocatalytic approach, utilizing a bifunctional squaramide-based catalyst. It enables the precise synthesis of chiral spirooxindole-tetrahydroquinazolines with intricate structures, featuring chiral quaternary centers.
View Article and Find Full Text PDFRing-fused aminal is an interesting structural skeleton in biologically active and pharmaceutically relevant compounds. A novel and efficient method for synthesizing benzosulfamidate-fused tetrahydroquinazolines is described. By employing the [4+2]-cycloaddition of 2-aminophenyl enones with cyclic N-sulfimines in the presence of DMAP as a base, the desired benzosulfamidate-fused tetrahydroquinazolines were obtained in good yields with high diastereoselectivities.
View Article and Find Full Text PDFAn alcohol-induced blackout suggested to be related to a rapid increase in blood alcohol concentration and it is closely related to long-term memory creation. Blackout has been experienced by 35% of the general population and over 50% of university student population. In addition, it has been shown that blackout could be a precursor of injury risk.
View Article and Find Full Text PDFA novel and streamlined approach to synthesizing benzotriazepin-1-ones has been developed through a hexafluoroisopropanol-promoted decarboxylative cascade reaction between isatoic anhydrides and hydrazonoyl chloride. The [4 + 3] annulation of hexafluoroisopropyl 2-aminobenzoates with nitrile imines, generated in situ, is a key feature of this innovative reaction. This approach has offered a simple and efficient method for synthesizing a broad range of structurally intricate and highly functional benzotriazepinones.
View Article and Find Full Text PDFAn innovative and efficient approach has been developed for the synthesis of 5,6-dihydropyrazolo[5,1-]isoquinolines. This one-pot tandem reaction involves the reaction of ,-cyclic azomethine imines with α,β-unsaturated ketones, using KCO as the base and DDQ as the oxidant. The process results in functionalized 5,6-dihydropyrazolo[5,1-]isoquinolines with good yields.
View Article and Find Full Text PDFThe first base-mediated [4 + 2] annulation of δ-hydroxy-α,β-unsaturated ketones with azlactones has been developed, through which 3,4-disubstituted 3-amino-δ-lactones were obtained in good yields and with excellent diastereoselectivities. This approach was also applied to the [4 + 2] annulation of δ-sulfonamido-α,β-unsaturated ketones, which provided a practical protocol for constructing biologically important 3-amino-δ-lactam frameworks.
View Article and Find Full Text PDFAlthough vitamin D (VD; serum 25 hydroxyvitamin D) deficiency (< 20Â ng/mL) is widespread among Japanese women, the VD status among pregnant women is unknown. This study aimed to determine the VD status of pregnant Japanese women during different meteorological seasons and to determine the factors controlling VD status. A total of 309 pregnant Japanese women were recruited at 28 weeks of gestation at the gynecology department of a university hospital in Tokyo between August 2018 and October 2019.
View Article and Find Full Text PDF1,3-Dipolar cycloadditions of ,-cyclic azomethine imines with γ-NHTs-α,β-unsaturated ketones were developed to synthesize tricyclic dinitrogen-fused heterocycles. Highly functionalized tricyclic tetrahydroisoquinolines were readily obtained in good to high yields in the [3 + 2]-cycloaddition reaction of -Bz-protected ,-cyclic azomethine imines with γ-NHTs-α,β-unsaturated ketones under mild reaction conditions. Moreover, DABCO-catalyzed cycloaddition of -Ts-protected ,-cyclic azomethine imines with γ-NHTs-α,β-unsaturated ketones followed by cleavage of the tosyl group is a convenient route to synthesize tetrahydropyrazolo [5,1-]isoquinolines in good yields with excellent diastereoselectivities.
View Article and Find Full Text PDFThe first organocatalytic asymmetric [3 + 2]-annulation of γ-sulfonamido-α,β-unsaturated ketones with cyclic -sulfimines has been developed, and enantioenriched functionalized polyheterotricyclic imidazolidines were obtained in good yields and with excellent enantioselectivities. This approach was also extended to the asymmetric [3 + 2]-annulation of γ-hydroxy-α,β-unsaturated ketones, affording enantioenriched polyheterotricyclic oxazolidines. In addition, base-catalyzed [3 + 2]-annulations of γ-sulfonamido/γ-hydroxy-α,β-unsaturated ketones with cyclic -sulfimines were re-investigated under mild reaction conditions for the synthesis of racemic polyheterotricyclic imidazolidines and oxazolidines with excellent diastereoselectivities.
View Article and Find Full Text PDFJuntendo Iji Zasshi
September 2022
Objectives: Postoperative venous thromboembolism is an important peri-operative complication associated with total hip arthroplasty (THA). In particular, early detection of deep venous thrombosis (DVT) is important for the prevention of pulmonary embolism (PE). However, the methods and timing of examinations for DVT detection differ among the facilities.
View Article and Find Full Text PDFWe investigated the effect of black sticky rice with giant embryo (BSRGE) extract known to contain high levels of gamma-aminobutyric acid (GABA) on alcohol cravings in social drinkers. A total of 41 subjects were divided into a BSRGE extract group (G group:  = 21) and a placebo group (P group:  = 20), and a randomized placebo-controlled experiment was performed for 12 weeks. The G group took the BSRGE extracts that contained 30 mg of GABA per day.
View Article and Find Full Text PDFIntroduction: Both hemiarthroplasty (HA) and total hip arthroplasty (THA) are widely accepted surgical procedures for hip replacement following displaced femoral neck fractures. However, in cases involving an intact joint line before surgery, the choice between HA and THA remains debatable. This study investigated the prevalence of acetabular cartilage and labral abnormalities in elderly patients with femoral neck fractures.
View Article and Find Full Text PDFBisphosphonate treatment has known effects of improving bone mineral density and preventing fractures in children with steroid-induced osteoporosis. However, there have been reports that high-dosage pamidronate therapy induces osteopetrosis in the borders of bones. A 10-year-old boy undergoing long-term treatment with oral alendronate developed frequent fractures throughout adolescence while playing basketball.
View Article and Find Full Text PDFClin Psychopharmacol Neurosci
May 2022
Objective: Capsaicin, the pungent analgesic substance of hot peppers which produces a burning sensation and pain is known to affect Substance P and central opioid activities. This experiment was designed to test the effect of capsaicin on alcohol consumption in C57BL/6 and DBA/2 mice. These two strains are known to differ in both their alcohol consumption and their endogenous opioid distribution and response to alcohol.
View Article and Find Full Text PDFThe effects of auto-BT in primary TKA on the perioperative hemoglobin (Hb) concentration and mid-term health outcomes are unknown. This study was performed to analyze the detailed changes in the perioperative Hb concentration before and after the operation (days 0-14 postoperatively), cardiovascular events, and mortality rate within 1 and 5 years postoperatively. One hundred patients undergoing primary TKA with auto-BT using 800 mL of preoperatively collected blood at the authors' institution were included.
View Article and Find Full Text PDFJ Public Health (Oxf)
December 2021
Background: The purpose of this study is to investigate the drinking behavior of Korean pregnant women in 2017 and to compare the changes of drinking status with the results of the research conducted in 1997 and 2008.
Methods: Pregnant women at one obstetrics and gynecology hospital and one university hospital were the subjects of the study. They were filled out questionnaire.
Organocatalytic enantioselective intramolecular oxa-Michael reactions of benzyl alcohol bearing α,β-unsaturated carbonyls as Michael acceptors are presented herein. Using cinchona squaramide-based organocatalyst, enones as well as α,β-unsaturated esters containing benzyl alcohol provided their corresponding 1,3-dihydroisobenzofuranyl-1-methylene ketones and 1,3-dihydroisobenzofuranyl-1-methylene esters in excellent yields with high enantioselectivities. In addition, enantioenriched 1,3-dihydroisobenzofuranyl-1-methylene ketone could be obtained from the Wittig/oxa-Michael reaction cascade of 1,3-dihydro-2-benzofuran-1-ol.
View Article and Find Full Text PDFMost surgical treatment options for metastatic acetabular lesions involve variants of total hip arthroplasty (THA). However, these are technically complex reconstructions performed in very frail patients, and previous reports indicate complications such as dislocation, deep infection, aseptic loosening, and intraoperative death. A 73-year-old man presented to the emergency department at our hospital with right hip pain following a fall.
View Article and Find Full Text PDFBackground: The intercondylar roof line is one of the indicators used during anterior cruciate ligament (ACL) reconstruction to see the relation to the position of the tibial tunnel. The tibial tunnel can be made posteriorly in the anteriorly subluxated tibia. During ACL reconstruction, the tibiofemoral relationship of the opposite or normal knee should be considered.
View Article and Find Full Text PDFInt Clin Psychopharmacol
November 2020
Medication is integral in treating alcohol use disorder. However, because of the small to medium effect size, much effort is being exerted to identify predicting factors for effective pharmacological treatment in alcohol abuse disorder. Rather than focusing on abstinence days, alcohol craving, or frequency of drinking, which has been the focus of previous studies.
View Article and Find Full Text PDFCatalyst-free and mild synthetic methods for the construction of hindered α-amino acid derivatives are presented herein. A wide range of hindered amino acid amides can be readily obtained from the reaction of α-halohydroxamates with a variety of amines, including anilines, primary amines, and secondary amines. Moreover, the aza/aza-[4+3] cycloaddition of in situ-generated aza-oxyallyl cations with 2-aminophenyl α,β-unsaturated carbonyls to furnish seven-membered benzodiazepin-3-ones is reported for the first time.
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