Search results for "ToP"
showing 10 items of 17685 documents
Thiazole Analogues of the Marine Alkaloid Nortopsentin as Inhibitors of Bacterial Biofilm Formation
2020
Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 a…
Synthesis and anticancer activity of new thiazole nortopsentin analogues
2015
Carboxylate catalyzed isomerization of β,γ‐unsaturated N-acetylcysteamine thioesters
2022
We demonstrate herein the capacity of simple carboxylate salts – tetrametylammonium and tetramethylguanidinium pivalate – to act as catalysts in the isomerization of β,γ-unsaturated thioesters to α,β-unsaturated thioesters. The carboxylate catalysts gave reaction rates comparable to those obtained with DBU, but with fewer side reactions. The reaction exhibits a normal secondary kinetic isotope effect ( k 1H / k 1D = 1.065±0.026) with a β,γ−deuterated substrate. Computational analysis of the mechanism provides a similar value ( k 1H / k 1D = 1.05) with a mechanism where γ-reprotonation of the enolate intermediate is rate determining. peerReviewed
Synthesis, antiproliferative activity, and in silico insights of new 3-benzoylamino-benzo[ b ]thiophene derivatives
2014
A new series of 3-benzoylamino-5-imidazol-5-yl-benzo[b]thiophenes and the parent amino derivatives were synthesized and screened as antitumor agents. All tested compounds showed concentration-dependent antiproliferative activity profile against HeLa cell line, exhibiting GI50 values in the low micromolar range. The most active compounds were tested in cell cycle perturbation experiments. A rapid accumulation of cells in the G2/M phase, with a concomitant reduction of cells in both the S and G0/G1 phases, was observed, suggesting that cell exposure to selected derivatives produces mitotic failure. To rationalize the biological results, the 3-benzoylamino-benzo[b]thiophenes were analyzed thro…
Can adjunctive corticosteroid therapy improve patient-centered outcomes following third molar surgery? A systematic review
2021
Third molar surgery is frequently associated with postoperative discomfort such as pain, edema and trismus. We aimed to evaluate the current evidence on the efficacy of adjunctive corticosteroid therapy in improving patient-centered outcomes following third molar surgery.This systematic review assessed and searched PubMed, Google scholar, Scopus, web of science, clinicaltrials.gov and Cochrane central for controlled trials, up to May 2021. The primary outcome measures were patient-centered outcomes such as quality of life following the use of adjunctive corticosteroid therapy in third molar removal. Only randomized controlled trials published in English language were included.A total of 355…
QCD NLO with Powheg matching and top threshold matching in WHIZARD
2016
We present the status of the automation of NLO processes within the event generator WHIZARD. The program provides an automated FKS subtraction and phase space integration over the FKS regions, while the (QCD) NLO matrix element is accessed via the Binoth Les Houches Interface from an externally linked one-loop program. Massless and massive test cases and validation are shown for several e+e- processes. Furthermore, we discuss work in progress and future plans. The second part covers the matching of the NRQCD prediction with NLL threshold resummation to the NLO continuum top pair production at lepton colliders. Both the S-wave and P-wave production of the top pair are taken into account in t…