The Changing Landscape for Stroke\ua0Prevention in AF: Findings From the GLORIA-AF Registry Phase 2

Background GLORIA-AF (Global Registry on Long-Term Oral Antithrombotic Treatment in Patients with Atrial Fibrillation) is a prospective, global registry program describing antithrombotic treatment patterns in patients with newly diagnosed nonvalvular atrial fibrillation at risk of stroke. Phase 2 began when dabigatran, the first non\u2013vitamin K antagonist oral anticoagulant (NOAC), became available. Objectives This study sought to describe phase 2 baseline data and compare these with the pre-NOAC era collected during phase 1. Methods During phase 2, 15,641 consenting patients were enrolled (November 2011 to December 2014); 15,092 were eligible. This pre-specified cross-sectional analysis describes eligible patients\u2019 baseline characteristics. Atrial fibrillation disease characteristics, medical outcomes, and concomitant diseases and medications were collected. Data were analyzed using descriptive statistics. Results Of the total patients, 45.5% were female; median age was 71 (interquartile range: 64, 78) years. Patients were from Europe (47.1%), North America (22.5%), Asia (20.3%), Latin America (6.0%), and the Middle East/Africa (4.0%). Most had high stroke risk (CHA2DS2-VASc [Congestive heart failure, Hypertension, Age  6575 years, Diabetes mellitus, previous Stroke, Vascular disease, Age 65 to 74 years, Sex category] score  652; 86.1%); 13.9% had moderate risk (CHA2DS2-VASc = 1). Overall, 79.9% received oral anticoagulants, of whom 47.6% received NOAC and 32.3% vitamin K antagonists (VKA); 12.1% received antiplatelet agents; 7.8% received no antithrombotic treatment. For comparison, the proportion of phase 1 patients (of N = 1,063 all eligible) prescribed VKA was 32.8%, acetylsalicylic acid 41.7%, and no therapy 20.2%. In Europe in phase 2, treatment with NOAC was more common than VKA (52.3% and 37.8%, respectively); 6.0% of patients received antiplatelet treatment; and 3.8% received no antithrombotic treatment. In North America, 52.1%, 26.2%, and 14.0% of patients received NOAC, VKA, and antiplatelet drugs, respectively; 7.5% received no antithrombotic treatment. NOAC use was less common in Asia (27.7%), where 27.5% of patients received VKA, 25.0% antiplatelet drugs, and 19.8% no antithrombotic treatment. Conclusions The baseline data from GLORIA-AF phase 2 demonstrate that in newly diagnosed nonvalvular atrial fibrillation patients, NOAC have been highly adopted into practice, becoming more frequently prescribed than VKA in Europe and North America. Worldwide, however, a large proportion of patients remain undertreated, particularly in Asia and North America. (Global Registry on Long-Term Oral Antithrombotic Treatment in Patients With Atrial Fibrillation [GLORIA-AF]; NCT01468701

<i>In vitro</i> antimycobacterial and antimicrobial activity of some new pyrazoline, isoxazole and benzodiazepine derivatives containing 1,3,5-triazine nucleus <i>via</i> chalcone series

1277-1287In the present study, three new combinatorial libraries of substituted phenyl pyrazoline 5a-e, isoxazole 6a-e and 1,5-benzodiazepine 7a-e derivatives have been synthesised via the reaction of chalcone 4a-e with phenylhydrazine hydrochloride, hydroxylamine hydrochloride and o-phenylenediamine respectively. The structures of all the newly synthesised compounds have been assigned on the basis of FTIR, 1H and 13C NMR, LC-MS, and elemental analysis. The title compounds have been screened for their preliminary in vitro antimicrobial activity against a panel of pathogenic strains S. aureus, S. pyogenus, E. coli, P. aeruginosa, C. albicans, A. niger and A. calavatus. Most of the compounds show appreciable antimicrobial activity against the tested strains. Compounds 8b, 8c, 9b, 9d, and 9f are considered as the best desired bioactive antimicrobial analogues of the series. In vitro antimycobacterial activity for all the synthesised compounds has been carried out against Mycobacterium tuberculosis H37 Rv. Compounds 5a, 6d and 7b display promising antimycobacterial activity

Synthesis and characterization of some novel isoxazoles and 1,5-benzothiazepines bearing s-triazine nucleus

473-476The title compounds 7a-d and 8a-d have been prepared starting from chalcones 6a-d having s-triazine nucleus. These chalcones 6a-d on cyclisation with hydroxylamine hydro- chloride in presence of alkali and 2-aminothiophenol in presence of a few drops of glacial acetic acid give isoxazoles 7a-d and 1,5-benzothiazepines 8a-d respectively. All the products have been characterized by elemental analysis, IR, 1H NMR and LCMS data

Synthesis and studies of some novel s-triazine based aminopyrimidines, isoxazoles and 1,5-benzothiazepines

1707-1712An elegant synthesis of the titled compounds 7a-e, 8a-e and 9a-e have been presented starting from chalcones 6a-e based on s-triazine nucleus. These chalcones 6a-e on cyclisation with guanidine nitrate and hydroxylamine hydrochloride in the presence of alkali give aminopyrimidines 7a-e and isoxazoles 8a-e respectively. Further these chalcones 6a-e on cyclisation with 2-aminothiophenol in the presence of few drops of glacial acetic acid give 1,5-benzothiazepines 9a-e. All the products obtained from these reactions are characterized by elemental analysis, IR, ¹H NMR and mass spectral data

Poly(D,L-Lactide-Co-Glycolide) microspheres containing 5-fluorouracil: Optimization of process parameters

The objective of this research was to optimize the processing parameters for poly(D,L-lactide-coglycolide) (PLGA) microspheres of 5-fluorouracil (5-FU) and to mathematically relate the process parameters and properties of microspheres. Microspheres were prepared by a water-in-oil-in-water emulsion solvent evaporation technique. A 32 factorial design was employed to study the effect of the volume of the internal phase of the primary emulsion and the volume of the external phase of the secondary emulsion on yield, particle size, and encapsulation efficiency of microspheres. An increase in the volume of the internal phase of the primary emulsion resulted in a decrease in yield and encapsulation efficiency and an increase in particle size of microspheres. When the volume of the external phase of the secondary emulsion was increased, a decrease in yield, particle size, and encapsulation efficiency was observed. Microspheres with good batch-to-batch reproducibility could be produced. Scanning electron microscopic study indicated that microspheres existed as aggregates