Vestergaardlaursen9463
We report here a series of glucosides which are active as inhibitors of the angiotensin converting enzyme (ACE). They are structurally related to the natural compound eugenol and exhibited significant inhibition values. Their syntheses were expeditious and we could obtain informative docking plots of them complexed to this enzyme. A glucoside derived from eugenol, carrying a carboxylic group in the aglycone, was the most active of them (with an IC50 of 0.4 mM) and showed good binding energies in docking studies with ACE. Moreover, computational prediction of toxicity risks, physicochemical properties and drug score show that the glucoside derivative of eugenol is a suitable compound for optimisation studies aimed at finding new drug candidates.Background The aim of the present work was to set-up compounds that are able to act simultaneously as antimalarial and antioxidants. Trolox, a known antioxidant was chosen as a core structure to ensure the antioxidant activity and contribute to antiplasmodial effect. Results Ten compounds were prepared in one step and evaluated on chloroquino-sensitive (3D7) and chloroquino-resistant (FcB1) strains of Plasmodium falciparum. The most active compound (3d) shows antiplasmodial activity in the range of chloroquine against chloroquino-sensitive and chloroquino-resistant P. falciparum strain. The antioxidant activity of (3d) was conducted through four tests and was found to be more potent than trolox itself and L-ascorbic acid. Conclusion Compound (3d) can be considered as an excellent lead molecule for further in vivo studies. This study paves the way for building large chemical libraries to be investigated in the field of malaria.
To assess the relative safety of oral tapentadol PR and other opioid analgesics for moderate or severe chronic pain in adults, we conducted a systematic review and network meta-analysis (NMA).
A systematic review was conducted to identify randomized controlled trials (RCTs) and randomized withdrawal trials of tapentadol with other WHO stage II and III opioid analgesics in patients with moderate or severe chronic pain. Searches were conducted in MEDLINE, EMBASE, PubMed, Cochrane databases and trial registries. Feasibility assessment evaluated the trials' suitability for NMA. Outcomes assessed were overall AEs, overall serious adverse events, constipation, nausea, dizziness, somnolence, headache, and discontinuation due to AEs. Randomized withdrawal trials were analyzed separately to other RCTs.
Searches conducted in April 2019 identified 16,604 records. Following screening and feasibility assessment, 29 RCTs and 19 randomized withdrawal trials were identified and included in the NMA. Consistent with existing research, evidence from RCTs suggested that tapentadol is associated with relatively lower odds of adverse events occurring than most active comparators. The withdrawal trial data were less clear, with higher uncertainty around the results, and results that appear to contradict the RCT evidence. There are a number of trial design factors that may be affecting these results.
RCT evidence suggests that tapentadol can be a useful treatment option for patients suffering from chronic pain and in need of an opioid analgesic. Opioids should be prescribed by a qualified physician only after other analgesics have been considered, taking side effects and misuse risk into account.
RCT evidence suggests that tapentadol can be a useful treatment option for patients suffering from chronic pain and in need of an opioid analgesic. Opioids should be prescribed by a qualified physician only after other analgesics have been considered, taking side effects and misuse risk into account.The natural tridecapeptide neurotensin has been emerged as a promising therapeutic scaffold for the treatment of neurological diseases and cancer. In this work, we aimed to identify the top 100 most cited original research papers as well as recent key studies related to neurotensins. The Web of Science Core Collection database was searched and the retrieved research articles were analyzed by using the VOSviewer software. The most cited original articles were published between 1973 and 2013. The top-cited article was by Carraway and Leeman reporting the discovery of neurotensin in 1973. The highly cited terms were associated with hypotension and angiotensin-converting-enzyme. The conducted analysis reveals the therapeutic potentials of neurotensin, and further impactful research toward its clinical development is warrantied.
The main aim of this study was to analyse the psychometric properties of the Polish version of the Multiple Sclerosis Self-Management-Revised Scale.
A total of 663 patients with multiple sclerosis were included in this study. read more The Polish version of the Multiple Sclerosis Self-Management-Revised Scale, The General Self-Efficacy Scale, Multiple Sclerosis Impact Scale-29, and Expanded Disability Status Scale were used. Cronbach's alpha and McDonald's omega coefficients were calculated to assess the Polish version of the scale's reliability. The reliability of the scale's test items was assessed using an information function with the multidimensional graded response model. Confirmatory factor and principal component analyses were conducted.
Cronbach's α and McDonald's ω were obtained (α = 0.896, ω = 0.909). Correlations between the scores of the Polish version of the Multiple Sclerosis Self-Management-Revised Scale and the General Self-Efficacy Scale (
= 0.34;
< 0.001) and the neurological assessments patients in Poland.
Using only the total score of the Multiple Sclerosis Self-Management-Revised Scale is recommended for Polish patients. The scale's factor structure requires further study. Implications for rehabilitation The Polish version of the Multiple Sclerosis Self-Management-Revised Scale was reliable and valid when used in adult multiple sclerosis patients. At present, we recommend using only the total score of the Multiple Sclerosis Self-Management-Revised Scale. Further research is needed to distinguish the detailed subscales of the Polish version of the tool. The Polish version of the Multiple Sclerosis Self-Management-Revised Scale can be used in clinical practice and for research purposes to assess the general level of self-management in Polish-speaking multiple sclerosis patients in Poland.