Search results for "IPR"
showing 10 items of 1515 documents
Simple dialkyl pyrazole-3,5-dicarboxylates show in vitro and in vivo activity against disease-causing trypanosomatids.
2017
SUMMARYThe synthesis and antiprotozoal activity of some simple dialkyl pyrazole-3,5-dicarboxylates (compounds 2–6) and their sodium salts (pyrazolates) (compounds 7–9) against Trypanosoma cruzi, Leishmania infantum and Leishmania braziliensis are reported. In most cases the studied compounds showed, especially against the clinically significant amastigote forms, in vitro activities higher than those of the reference drugs (benznidazole for T. cruzi and glucantime for Leishmania spp.); furthermore, the low non-specific cytotoxicities against Vero cells and macrophages shown by these compounds led to good selectivity indexes, which are 8–72 times higher for T. cruzi amastigotes and 15–113 tim…
Wear of the Primary WaveOne single file when shaping vestibular root canals of first maxillary molar
2017
Background It is very important for a clinician to know the increased wear of mechanized files when establishing endodontic therapy. The aim of this study was to check the wear of the Primary WaveOne file upon shaping two, four and six maxillary molar vestibular canals. Material and Methods The deterioration of 40 files, divided into four groups, was evaluated microscopically: group 1, control (unused); group 2, two canals; group 3, four canals; and group 4, six canals. After instrumentation, the files were embedded in resin and sectioned at their apical third into three equal parts. To analyze the wear of edges in the different sections, AutoCAD software was used and analysis of variance (…
SWhybrid: A Hybrid-Parallel Framework for Large-Scale Protein Sequence Database Search
2017
Computer architectures continue to develop rapidly towards massively parallel and heterogeneous systems. Thus, easily extensible yet highly efficient parallelization approaches for a variety of platforms are urgently needed. In this paper, we present SWhybrid, a hybrid computing framework for large-scale biological sequence database search on heterogeneous computing environments with multi-core or many-core processing units (PUs) based on the Smith- Waterman (SW) algorithm. To incorporate a diverse set of PUs such as combinations of CPUs, GPUs and Xeon Phis, we abstract them as SIMD vector execution units with different number of lanes. We propose a machine model, associated with a unified …
Multi-approach metabolomics analysis and artificial simplified phytocomplexes reveal cultivar-dependent synergy between polyphenols and ascorbic acid…
2017
Fruits of the sweet cherry (Prunus avium L.) accumulate a range of antioxidants that can help to prevent cardiovascular disease, inflammation and cancer. We tested the in vitro antioxidant activity of 18 sweet cherry cultivars collected from 12 farms in the protected geographical indication region of Marostica (Vicenza, Italy) during two growing seasons. Multiple targeted and untargeted metabolomics approaches (NMR, LC-MS, HPLC-DAD, HPLC-UV) as well as artificial simplified phytocomplexes representing the cultivars Sandra Tardiva, Sandra and Grace Star were then used to determine whether the total antioxidant activity reflected the additive effects of each compound or resulted from synergis…
Effects of Pimozide Derivatives on pSTAT5 in K562 Cells
2017
STAT5 is a transcription factor, a member of the STAT family of signaling proteins. STAT5 is involved in many types of cancer, including chronic myelogenous leukemia (CML), in which this protein is found constitutively activated as a consequence of BCR-ABL expression. The neuroleptic drug pimozide was recently reported to act as an inhibitor of STAT5 phosphorylation and is capable of inducing apoptosis in CML cells in vitro. Our research group has synthesized simple derivatives of pimozide with cytotoxic activity and that are able to decrease the levels of phosphorylated STAT5. In this work we continued the search for novel STAT5 inhibitors, synthesizing compounds in which the benzoimidazol…
Prospecting for cytotoxic and antiprotozoal 4-aryl-4H-chromenes and 10-aryldihydropyrano[2,3-f]chromenes.
2018
Different studies reported that genetic predisposition or metabolic dysfunction are the risk factors for cancer. Infectious parasitic diseases were listed among factors that predispose to cancer. Because of the resemblance between the life cycle of cancer cells and some parasites, this study aimed to prepare pyran derivatives with cytotoxic and antiprotozoal potencies. Therefore, 7 chromenes, 10 pyranocoumarins, and an unexpected intermediate were obtained from a multi-reagent one-pot reaction. These compounds were evaluated for their cytotoxicity on sensitive and resistant leukemia cancer cells lines and against two protozoan parasites, namely Trypanosoma cruzi and Leishmania amazonensis a…
Bistacrines as potential antitrypanosomal agents
2017
Human African Trypanosomiasis (HAT) is caused by two subspecies of the genus Trypanosoma, namely Trypanosoma brucei rhodesiense and Trypanosoma brucei gambiense. The disease is fatal if left untreated and therapy is limited due to only five non-adequate drugs currently available. In preliminary studies, dimeric tacrine derivatives were found to inhibit parasite growth with IC50-values in the nanomolar concentration range. This prompted the synthesis of a small, but smart library of monomeric and dimeric tacrine-type compounds and their evaluation of antiprotozoal activity. Rhodesain, a lysosomal cathepsin-L like cysteine protease of T. brucei rhodesiense is essential for parasite survival a…
Staphylococcus aureus bloodstream infection in patients with prosthetic joint included in the prospective VIRSTA cohort study: frequency and time of …
2019
International audience; Among 143 patients of the VIRSTA cohort study with Staphylococcus aureus bacteremia and an arthroplasty implanted for more than a year, S. aureus periprosthetic joint infection was observed in 19%. Signs of infection (pain and swelling) were always present, in median 1 day (range, 0-21 days) after onset of bacteremia. Staphylococcus aureus has both a high potential for metastatic infection and a high affinity for foreign material. Possible prosthesis infection is of clinical concern in all patients with preexisting prosthetic materials experiencing S. aureus bloodstream infection (SAB). Prosthetic joints are especially prone to infection during the course of bacterem…
Bayesian approach to urinary ESBL-producing Escherichia coli
2014
This is a retrospective study about the prevalence of ESBL-producing Escherichia coli (EEC) in urinary specimens from patients from the Comunitat Valenciana from January 2007 to December 2008. Data were retrieved from RedMIVA, and Bayesian generalized linear mixed models were considered to study the prevalence of EEC with regard to demographical and microbiological factors. The total number of infections considered was 164,502, the amount of urinary isolates was 70,827 belonging to 49,304 different patients, and 5,161 (7.3%) of the urinary isolates were EEC. Three out of four E. coli were isolated in women (76.8%), men showed higher rates of EEC (9.7% in men vs. 6.5% in women). EEC patients…
Synthesis and antiproliferative mechanism of action of pyrrolo[3′,2′:6,7] cyclohepta[1,2-d]pyrimidin-2-amines as singlet oxygen photosensitizers
2016
A new series of pyrrolo[3′,2′:6,7]cyclohepta[1,2-d]pyrimidin-2-amines, was conveniently prepared using a versatile and high yielding multistep sequence. A good number of derivatives was obtained and the cellular photocytotoxicity was evaluated in vitro against three different human tumor cell lines with EC50 (0.08–4.96 μM) values reaching the nanomolar level. Selected compounds were investigated by laser flash photolysis. The most photocytotoxic derivative, exhibiting a fairly long-lived triplet state (τ ∼ 7 μs) and absorbance in the UV–Vis, was tested in the photo-oxidations of 9,10-anthracenedipropionic acid (ADPA) by singlet oxygen. The photosentizing properties are responsible for the c…