Aerobic Copper-Promoted Oxidative Dehydrosulfurative Carbon-Oxygen Cross-Coupling of 3,4-Dihydropyrimidine-1: H -2-Thiones With Alcohols

An aerobic Cu-promoted oxidative dehydrosulfurative carbon-oxygen cross-coupling of 3,4-dihydropyrimidin-1H-2-thiones (DHPMs) with both aliphatic and aromatic alcohols is described. Together with the ready availability of DHPMs and both alcohols, the method furnishes facile access to biologically valuable 2-alkoxypyrimidines with rapid diversification

The Effects of Acupuncture Stimulation for Brain Activation and Alcohol Abstinence Self-Efficacy: Functional MRI Study

We attempted to investigate whether acupuncture stimulation at HT7 can have an effect on brain activation patterns and alcohol abstinence self-efficacy. Thirty-four right-handed healthy subjects were recruited for this study. They were randomly assigned into two groups: the HT7 (Shenmen) group and the LI5 (Yangxi) group. Acupuncture stimulation was performed using a block paradigm during fMRI scanning. Additionally, the Korean version of Alcohol Abstinence Self-Efficacy Scale (AASES) was used to determine the effect of acupuncture stimulation on self-efficacy to abstain from alcohol use. According to the result of fMRI group analysis, the activation induced by HT7 stimulation was found on the bilateral postcentral gyrus, inferior parietal lobule, inferior frontal gyrus, claustrum, insula, and anterior lobe of the cerebellum, as well as on the left posterior lobe of the cerebellum (p<0.001, uncorrected). According to the AASES analysis, the interaction effect for gender and treatment was marginally significant (F(1,30)=4.152, p=0.050). For female group, the simple main effect of treatment was significant (F(1,11)=8.040, p=0.016), indicating that the mean change score was higher in the HT7 stimulation than in the LI5 stimulation. Therefore, our study has provided evidence to support that HT7 stimulation has a positive therapeutic effect on the alcohol-related diseases

CTA-Based Truncal-Type Occlusion Is Best Matched With Postprocedural Fixed Focal Stenosis in Vertebrobasilar Occlusions

Background: Differentiation of embolic and atherosclerotic occlusions is difficult prior to endovascular treatment (EVT) of acute ischemic stroke due to intracranial large artery occlusions. CTA-determined occlusion type has been reported to be associated with a negative cardiac embolic source and stent retriever failure, a potential of intracranial atherosclerosis (ICAS)-related occlusions. In this study, we evaluated the agreement between preprocedural identification of CTA-determined truncal-type occlusion (TTO) and postprocedural evaluation of underlying fixed focal stenosis (FFS) in the occlusion site.Methods: Patients who underwent intracranial EVT for acute ischemic stroke within 24 h of onset and who had baseline CTA were identified from a multicenter registry collected between January 2011 and May 2016. Preprocedural occlusion type was classified as TTO (target artery bifurcation saved) or branching-site occlusion (bifurcation involved) on CTA. As for postprocedural identification, FFS was evaluated by stepwise analyses of procedural and postprocedural angiographies. The agreement between TTO and FFS was evaluated in respective intracranial vascular beds. Receiver operating characteristics analyses were also performed.Results: A total of 509 patients were included [intracranial internal carotid artery (ICA): 193, middle cerebral artery (MCA) M1: 256, and vertebrobasilar artery (VBA): 60]. In preprocedural identification, 33 (17.1%), 41 (16.0%), and 29 patients (48.3%) had TTOs, respectively. TTOs had good agreement with angiographic FFS in M1 (positive predictive value: 63.4%, negative predictive value: 83.2%, likelihood ratio: 5.42, Pmultivariate &lt; 0.001) and VBA (72.4%, 96.8%, and 4.54, respectively, Pmultivariate = 0.004), but not in intracranial ICA occlusions (Pmultivariate = 0.358). The area under the receiver operating characteristics curve was the largest for VBA (0.872, p &lt; 0.001), followed by MCA M1 (0.671, p &lt; 0.001), and intracranial ICA (0.551, p = 0.465).Conclusions: Agreement between preprocedural TTO and postprocedural FFS, both of which are surrogate markers for ICAS-related occlusions, is highest for VBA, followed by MCA M1 occlusions. There is no significant association in intracranial ICA

A Case of Non-Functioning Huge Adrenocortical Carcinoma Extending Into Inferior Vena Cava and Right Atrium

Primary adrenocortical carcinoma (ACC) is a rare tumor and its usual sites of metastasis are the lung (71%), lymph node (68%), liver (42%), and bone (26%). However, intracaval invasion extending into the right atrium is very rare and spontaneous regression of tumor burden in adrenal carcinoma is also rare. We report a case of ACC with direct invasion of the inferior vena cava and right atrium. A 34-yr-old male patient presented with progressive dyspnea, weight loss, and poor oral intake over 3 months. Non-functioning ACC with direct invasion of the inferior vena cava and right atrium was confirmed by imaging, pathologic, and hormonal study. Chemo-radio-therapy was attempted. However, tumor burden was not changed, but rather toxic hepatitis and thrombocytopenia were developed. His subjective symptoms and general conditions were improved after 1 month of conservative management and the patient was discharged. During clinical follow-up, this tumor showed spontaneous regression

Association Between Inappropriateness of Left Ventricular Mass and Left Ventricular Diastolic Dysfunction: A Study Using the Tissue Doppler Parameter, E/E'

Background and Objectives: The structural significance of the inappropriateness of left ventricular mass (iLVM) is known to be an important prognostic factor for cardiovascular events; however, the functional changes associated with iLVM have not been established. This study was performed to determine if diastolic dysfunction is associated with iLVM using a tissue Doppler technique. Subjects and Methods: Three hundred sixty consecutive subjects, including 221 hypertension patients from the echocardiography database, were analyzed. Regarding the appropriateness of left ventricular (LV) mass, an observed/predicted ratio of IV mass (OPR) > 130% was defined as inappropriate. Echocardiographic parameters, including early diastolic peak velocity (E)/late diastolic peak velocity (A), deceleration time (DT), isovolumetric relaxation time (IVRT), and E/early mitral annulus velocity (E'), were compared between the appropriate LV mass (aLVM) group and the iLVM group. Results: Among transmitral flow parameters, only the E velocity was negatively correlated with the OPR when adjusted for age (adjusted r=-0.107, p=0.04). Based on multiple regression analysis, the OPR (??=0.163, p=0.003), as well as age (??=0.286, p=0.0001), systolic blood pressure (??=0.120, p=0.019), fasting blood glucose (??=0.098, p=0.042), and male gender (??=0.157, p=0.002) were independent factors determining E/E'. The cholesterol level was not an independent factor (??=-0.059, p=0.355). In the iLVM group (n=105), the adjusted E/E' was higher than in the aLVM group (n=255; 11.7 ?? 3.4 vs. 10.8 ?? 3.1, p=0.02), while the peak E flow velocity was significantly lower than in the aLVM group (70.9 ?? 15.1 vs. 75.5 ?? 17.6, p=0.03). Conclusion: Inappropriateness of LV mass is independently associated with increased E/E'. Thus, E/E' may be a useful parameter for the evaluation of diastolic dysfunction. Copyright ?? 2009 The Korean Society of Cardiology

Antileishmanial High-Throughput Drug Screening Reveals Drug Candidates with New Scaffolds

Drugs currently available for leishmaniasis treatment often show parasite resistance, highly toxic side effects and prohibitive costs commonly incompatible with patients from the tropical endemic countries. In this sense, there is an urgent need for new drugs as a treatment solution for this neglected disease. Here we show the development and implementation of an automated high-throughput viability screening assay for the discovery of new drugs against Leishmania. Assay validation was done with Leishmania promastigote forms, including the screening of 4,000 compounds with known pharmacological properties. In an attempt to find new compounds with leishmanicidal properties, 26,500 structurally diverse chemical compounds were screened. A cut-off of 70% growth inhibition in the primary screening led to the identification of 567 active compounds. Cellular toxicity and selectivity were responsible for the exclusion of 78% of the pre-selected compounds. The activity of the remaining 124 compounds was confirmed against the intramacrophagic amastigote form of the parasite. In vitro microsomal stability and cytochrome P450 (CYP) inhibition of the two most active compounds from this screening effort were assessed to obtain preliminary information on their metabolism in the host. The HTS approach employed here resulted in the discovery of two new antileishmanial compounds, bringing promising candidates to the leishmaniasis drug discovery pipeline

Current distribution and current efficiency in pulsed current plating of nickel

A mathematical model is presented to obtain the current distribution and current efficiency on a rotating disk electrode under controlled current condition. The calculated results compare well with experiments performed using a nickel/nickel sulfate system in the presence of boric acid, The current density is highly nonuniform due to the ohmic drop in the electrolyte. The current efficiency was decreased with the increase of hydrogen concentration as well as applied pulse current density.clos

Initial Catalyst−Substrate Association Step in Enyne Metathesis Catalyzed by Grubbs Ruthenium Complex Probed by Time-Dependent Fluorescence Quenching

This communication introduces an FRET-based simple and efficient method for monitoring kinetics and thermodynamics of organic reactions and describes its application to studies on the initial catalyst-substrate association step in the enyne metathesis catalyzed by a Grubbs Ru complex to probe the reaction initiation on the alkyne versus the alkene. The kinetic and thermodynamic parameters of alkene and alkyne with the first generation Grubbs Ru complex, determined by the time-dependent fluorescence quenching of the dye-conjugated substrate by the Ru catalyst, strongly support the dominance of the reaction initiation on alkene over alkyne in the reaction both kinetically and thermodynamically.1122sciescopu

Endoscopic ultrasound-guided biliary drainage with placement of a fully covered metal stent for malignant biliary obstruction

AIM: To determine the utility of endoscopic ultrasound-guided biliary drainage (EUS-BD) with a fully covered self-expandable metal stent for managing malignant biliary stricture