Synthesis of thiazolyl hydrazonothiazolamines and 1,3,4‐thiadiazinyl hydrazonothiazolamines as a class of antimalarial agents

Novel thiazolyl hydrazonothiazolamines and 1,3,4‐thiadiazinyl hydrazonothiazolamines were synthesized by a facile one‐pot multicomponent approach by the reaction of 2‐amino‐4‐methyl‐5‐acetylthiazole, thiosemicarbazide or thiocarbohydrazide and phenacyl bromides or 3‐(2‐bromoacetyl)‐2H‐chromen‐2‐ones in acetic acid with good to excellent yields. These new compounds were screened in vitro for their antimalarial activity; among them, four compounds, 4h, 4i, 4k, 4l , showed moderate activity with half‐maximal inhibitory concentration (IC₅₀) values of 3.2, 2.7, 2.7, and 2.8 and 3.2, 3.2, 3.1, and 3.5 μM against chloroquine‐sensitive and ‐resistant strains of Plasmodium falciparum, respectively. Compound 4l inhibited the ring stage growth of P. falciparum 3D7 at an IC₉₀ concentration of 12.5 µM in a stage‐specific assay method, where the culture is incubated with specific stages of P. falciparum for 12 hr, and no activity was found against the trophozoite and schizont stages, confirming that 4l may have potent action against the ring stage of P. falciparum.     

Is video observation as effective as live observation in improving teamwork in the operating room?

Background

Teamwork in the operating room decreases the risk of preventable patient harm. Observation in the operating room allows for evaluation of compliance with best-practice surgical guidelines. This study examines the relative ability of video and live observation to promote operating room teamwork.

Effect of renal transplantation for chronic renal disease on left ventricular mass

Chronic kidney disease is associated with an increased left ventricular (LV) mass. Few data are available regarding the effect of renal transplantation on LV mass regression or the clinical factors associated with LV mass regression. Patients with ≥1 year of chronic kidney disease followed by successful renal transplantation were identified. All patients underwent echocardiography ≥6 months before transplantation with repeat echocardiography ≥1 year after transplantation. An experienced echocardiographer, who was unaware of the clinical data, performed all linear measurements in the parasternal long-axis projection, including systolic and diastolic LV chamber dimensions and LV wall thickness. The LV mass was calculated as follows: 0.8 × {1.04 [(LV internal dimension at end diastole + posterior wall thickness at end diastole + LV wall thickness at the cardiac base for the anteroseptum)(3) - (LV internal dimension at end diastole)(3)]} + 0.6 g. Candidate clinical variables for an association with LV mass regression were assembled, including age, gender, race, donor type, renal disease etiology, medications (insulin, oral hypoglycemics, antihypertensives, statins, and antirejection medications), and co-morbidities. Patients were separated into 2 groups according to presence and absence of LV mass regression. A total of 105 patients (mean age 54 years; 58 men) were included in the study with a mean follow-up of 1.7 years. Of the 105 patients, 57 had significant LV mass regression (mean difference -37.2 ± 31.3 g/m(2)) and 48 had no significant regression (mean difference 15.7 ± 17.1 g/m(2)). The extent of the LV mass before transplantation was the only predictor of mass regression after transplantation (odds ratio 1.50, 95% confidence interval 1.26 to 1.80). In conclusion, significant LV mass regression is present in most patients after renal transplantation. The extent of the LV mass before transplantation was the only clinical predictor of regression.