Potential for Aedes aegypti Larval Control and Environmental Friendliness of the Compounds Containing 2-Methyl-3,4-dihydroquinazolin-4-one Heterocycle.

2-Methylquinazolin-4(3H)-one was prepared by the reaction of anthranilic acid, acetic anhydride, and ammonium acetate. The reaction of 2-methylquinazolin-4(3H)-one with N-aryl-2-chloroacetamides in acetone in the presence of potassium carbonate gave nine N-aryl-2-(2-methyl-4-oxoquinazolin-3(4H)-yl)acetamide compounds. The structures of these compounds were elucidated on the basis of their IR, 1H nuclear magnetic resonance (NMR), 13C NMR, and high-resolution mass spectrometry (HR-MS) spectral data. These synthesized compounds containing the 2-methyl-3,4-dihydroquinazolin-4-one moiety exhibited activity against Aedes aegypti mosquito larvae with LC50 values of 2.085-4.201 µg/mL after 72 h exposure, which is also confirmed using a quantitative structure-activity relationship (QSAR) model. Interestingly, these compounds did not exhibit toxicity to the nontarget organism Diplonychus rusticus. In silico molecular docking revealed acetylcholine binding protein (AChBP) and acetylcholinesterase (AChE) to be potential molecular targets. These data indicated the larvicidal potential and environmental friendliness of these N-aryl-2-(2-methyl-4-oxoquinazolin-3(4H)-yl)acetamide derivatives.

Pulmonary Artery Diameter (PAD) and the Pulmonary Artery to Aorta Ratio (PAD/AAD) as Assessed by Non-contrast Cardiac CT: The Association with Left Ventricular (LV) Remodeling and the LV Function.

Objective Dilatation of the pulmonary artery itself (PAD: pulmonary artery diameter) or in relation to the ascending aorta (PAD/AAD: pulmonary artery diameter to ascending aortic diameter ratio) has been reported to be associated with pulmonary hypertension and with a prognostic outcome of either heart failure or cardiovascular events. We herein aimed to assess the correlations between pulmonary hypertension-related parameters PAD (or PAD/AAD) and left ventricular (LV) remodeling and LV function. Methods This retrospective study included 193 patients (ages: 67±12 years) who underwent both coronary CT angiography (CCTA) and echocardiography. The PAD and the AAD were measured on a transaxial non-contrast CCTA image at the level of the pulmonary artery bifurcation. Left ventricular mass (LVM), relative wall thickness ratio (RWT), left ventricular ejection fraction (LVEF), left atrial volume (LAV), and early mitral inflow velocity to mitral annular early diastolic velocity ratio (E/e') were evaluated by echocardiography. The relationships between PAD (or PAD/AAD) and echocardiography parameters were assessed, and adjusted for the demographic data and cardiovascular disease (CVD) risk factors by a multivariable linear regression analysis. Results PAD (mean±SD: 2.6±0.4 cm) was positively correlated with LVM (r=0.34, p<0.001), LAV (r=0.41, p<0.001), and E/e' (r=0.29, p<0.001). PAD/AAD (mean±SD: 0.76±0.12 cm) was positively correlated with LVM (r=0.12, p=0.09), LAV (r=0.24, p<0.001), and E/e' (r=0.15, p=0.04). These correlations remained significant after adjusting for demographic data and CVD risk factors. PAD (or PAD/AAD) did not correlate with LVEF or RWT (p>0.05). Conclusion Greater PAD or PAD/AAD is significantly associated with LV remodeling and an impaired LV function.

A green approach for the synthesis of 2-substituted benzoxazoles and benzothiazoles via coupling/cyclization reactions.

We have developed the green method for the synthesis of benzoxazoles and benzothiazoles with moderate to good yields using imidazolium chlorozincate (II) ionic liquid supported into Fe3O4 nanoparticles (LAIL@MNP) under solvent-free sonication. The reaction was performed under mild conditions and only produced water as a sole byproduct. The reactions under solvent-free sonication showed advantages of faster reaction rate (30 min) and high yields of the products (up to 90%). Moreover, the LAIL@MNP material was easily separated from the reaction mixture and can be recycled for five consecutive runs with a slight decrease in its catalytic performance (from 82 to 73%).

Synthesis of a new series of 2-hydroxy-5-iodo-N'-(1-arylethylidene)benzohydrazides using a deep eutectic solvent as solvent/catalyst under sonication.

We report here the preparation of 2-hydroxy-5-iodo-N'-(1-arylethylidene)benzohydrazide compounds in good to excellent yields (83-98%) within a short reaction time (10-15 min), through a clean and efficient procedure. Seventeen new compounds were synthesized and fully characterized by FT-IR, NMR, and HRMS. The deep eutectic solvent can be recovered easily by phase extraction and can be reused up to several times without any significant loss of catalytic activity. Additionally, the method has a wide substrate scope and provides an accessible route for the large-scale direct synthesis of 2-hydroxy-5-iodo-N'-(1-arylethylidene)benzohydrazides.

Early prediction of triple negative breast cancer response to cisplatin treatment using diffusion-weighted MRI and 18F-FDG-PET.

BACKGROUND: We evaluated the potential of diffusion-weighted MRI (DW-MRI) and 18F-FDG-PET for the early prediction of a triple negative breast cancer (TNBC) response to cisplatin. METHODS: Cisplatin-treated TNBC tumor-bearing mice were categorized as responders or non-responders based on the tumor growth rate. DW-MRI and 18F-FDG-PET were performed before and after treatment (day 0 and days 3 and 7, respectively). The average apparent diffusion coefficient value (ADCmean), the highest standardized uptake value (SUVmax), and the metabolic tumor volume (MTV) were measured. The ratios of each parameter relative to day 0 were calculated [ΔADCmean (day 3) and (day 7), ΔSUVmax (day 3) and (day 7), and ΔMTV (day 3) and (day 7), respectively]. Overall survival rates were compared based on the thresholds determined by these parameters. RESULTS: Both the day 3 and day 7 ratios of ADCmean and MTV showed significant differences between the responder and non-responder groups, whereas the ratios of SUVmax did not. Mice with ΔADCmean (day 3) exceeding the threshold showed a longer overall survival rate. Mice with ΔSUVmax (day 7), ΔMTV (day 3), and ΔMTV (day 7) below the respective thresholds showed a longer overall survival rate. CONCLUSIONS: The ratios of ADCmean, SUVmax, and MTV have the potential to predict the therapeutic response and to screen non-responders in the ultra-early phase following cisplatin treatment in patients with TNBC.

Association of Aortic Arch Width Assessed by Noncontrast Cardiac Computed Tomography With Cardiac Remodeling, Cardiac Function, and Atherosclerosis in a Japanese Cohort.

PURPOSE: Age-related aortic changes are related to adverse cardiac remodeling and reduced cardiac function. Here, we aim to assess the correlations between aortic arch width (AAW) and left ventricular (LV) remodeling and LV function as well as coronary artery calcification (CAC). MATERIALS AND METHODS: This retrospective study included 194 patients (ages, 67±12 y) who underwent both coronary computed tomography angiography and echocardiography. The AAW is defined as the longest width between the ascending and descending aorta on a transaxial noncontrast coronary computed tomography angiography image at the level of the pulmonary artery bifurcation. Left ventricular mass, relative wall thickness ratio, left ventricular ejection fraction, left atrial volume, and early mitral inflow velocity to mitral annular early diastolic velocity ratio (E/e') were evaluated by echocardiography. CAC was assessed by Agatston score. The relationships between AAW and echocardiography parameters were assessed, and adjusted for demographic data and cardiovascular disease risk factors by multivariate linear regression analysis. RESULTS: AAW (mean±SD, 11.6±1.4 cm) was positively correlated with left ventricular mass (r=0.28, P<0.0001), left atrial volume (r=0.28, P<0.0001), and E/e' (r=0.21, P<0.01). These correlations remained significant after adjustment for demographic data and cardiovascular disease risk factors. There was no correlation between AAW and left ventricular ejection fraction or relative wall thickness. There was a significant difference of AAW between the groups with Agatston score <100 and those with Agatston score ≥100, and this difference persisted after adjustment for all covariates (P<0.01). CONCLUSION: Greater AAW was significantly associated with LV remodeling and impaired function as well as advanced CAC.