Recent developments in the synthesis of novel xanthone-1,2,3-triazole dyads

The development of multi-target drugs for treating complex multifactorial diseases constitutes an active research ield. This kind of drugs has gained much importance as alternative strategy to combination therapy (“cocktail drugs”).1 A common way to design them brings together two different pharmacophores in one single molecule (so-called dyads). Following this idea and being aware that xanthones2 and 1,2,3-triazoles3 possess important pharmacological properties, we combined these two heterocycles in one molecule to create new dyads with improved therapeutic potential. In this work, new xanthone-1,2,3-triazole dyads were prepared from novel (E)-2-(4-arylbut-1-en-3-yn-1-yl)chromones by two different approaches to evaluate their eficiency and sustainability. Both methodologies involved Diels-Alder reactions to build the xanthone core, which were optimized using microwave irradiation as alternative heating method, and 1,3-dipolar cycloadditions to insert the 1,2,3-triazole moiety (Figure 1).4 All final and intermediate compounds were fully characterized by 1D and 2D NMR techniques.

Aerobic performance and morphological modifications after a 4 month physical activity training program in elderly women

Research clearly shows that physical activity (PA) is an important factor to develop and maintain good health and adequate body functions in older people. In this context, the purpose of this study was to determine aerobic performance and morphological modifications after a 4 month physical activity program (PAP) in elderly. METHODS Forty subjects divided in two groups (control, n=20; and experimental, n=20) were evaluated twice, at the beginning and after a 4-month-activity program period. This program called “+ age + health” consists of 3 week sessions of one hour each, based on walking and aerobic exercises. The control group had, at its first evaluation, the followings characteristics: average body mass 68kg±15, 28±5 BMI, 37%±5 body fat, 2.2kg±0.4 bone mass, 42%±9 lean body mass and did 129 repetitions ± 46 on a 2-Minute Step Test (2MST). The assessment of anthropometric and morphological variables was measured through an electrical bioimpedance scale (TANITA - BC 545). Aerobic endurance was evaluated from a 2MST.RESULTS In the control group only the percentage of body fat changed significantly, and increased over time. In the experimental group we found a positive relationship between PAP and the majority of morphological variables. The percentage of variation changed in: body fat (-4.3%±7.6, p=0.014), bone mass (2.4%±3.1, p=0.004) and 2MST (33.6%±63.1, p=0.023). In the remaining variables there were no significant modifications. The significant modification in 2MST after the activity period means that the aerobic performance can be improved in elderly, and attenuates the negative effects of age. Moreover, the benefits of PAP can be seen by positive alterations registered in lean body mass and in the percentage of body fat.