Background: Up to 25% of patients suffering from an acute stroke are diagnosed with delirium during the hospital stay, with older age increasing the risk. Generalized slowing in the electroencephalogram (EEG) supports the diagnosis of delirium. We examined the potential of single-channel EEG (DeltaScan) as an easy-to-use device on intensive care units for detecting delirium.
View Article and Find Full Text PDFThis article is a history of an industrial-academic partnership that started almost two decades ago and details the evolution of a relationship between a small academic research group and a spin-out company located in Portugal. Their activities have ranged from the development of new metal-based catalytic systems for asymmetric epoxidations, allylic alkylations, and arylations to the development of novel cinchona-based organocatalysts for asymmetric hydrosilylations and Michael additions. Current common interests are centered on the development of novel chiral Natural Deep Eutectic Solvent systems, which they are investigating in different types of reaction systems.
View Article and Find Full Text PDFEssential tremor (ET) amplitude is modulated by visual feedback during target driven movements and in a grip force task. It has not been examined yet whether visual feedback exclusively modulates target force tremor amplitude or if other afferent inputs like auditory sensation has a modulatory effect on tremor amplitude as well. Also, it is unknown whether the enhanced sensory feedback causes an increase of arousal in persons with ET (p-ET).
View Article and Find Full Text PDFMicrostate sequences summarize the changing voltage patterns measured by electroencephalography, using a clustering approach to reduce the high dimensionality of the underlying data. A common approach is to restrict the pattern matching step to local maxima of the global field power (GFP) and to interpolate the microstate fit in between. In this study, we investigate how the anesthetic propofol affects microstate sequence periodicity and predictability, and how these metrics are changed by interpolation.
View Article and Find Full Text PDFEEG microstate sequence analysis quantifies properties of ongoing brain electrical activity which is known to exhibit complex dynamics across many time scales. In this report we review recent developments in quantifying microstate sequence complexity, we classify these approaches with regard to different complexity concepts, and we evaluate excess entropy as a yet unexplored quantity in microstate research. We determined the quantities entropy rate, excess entropy, Lempel-Ziv complexity (LZC), and Hurst exponents on Potts model data, a discrete statistical mechanics model with a temperature-controlled phase transition.
View Article and Find Full Text PDFTransition-metal-catalyzed asymmetric reactions have been a powerful tool in organic synthesis for many years. The design of chiral ligands with the right configuration is fundamental to induce high regio- and stereoselectivity to catalytic reactions and to achieve high turnover numbers and high yields. A challenge is the control of prochiral centers with similar electronic properties in a similar steric environment within the same molecule.
View Article and Find Full Text PDFThe inhibition of LTB(4) binding to and activation of G-protein-coupled receptors BLT1 and BLT2 is the premise of a treatment for several inflammatory diseases. In a lead optimization effort starting with the leukotriene B(4) (LTB(4)) receptor antagonist (2), members of a series of 3,5-diarylphenyl ethers were found to be highly potent inhibitors of LTB(4) binding to BLT1 and BLT2 receptors, with varying levels of selectivity depending on the substitution. In addition, compounds 33 and 38 from this series have good in vitro ADME properties, good oral bioavailability, and efficacy after oral delivery in guinea pig LTB(4) and nonhuman primate allergen challenge models.
View Article and Find Full Text PDFWe describe a novel series of potent inhibitors of the kinase activity of mTOR. The compounds display good selectivity relative to other PI3K-related kinase family members and, in cellular assays, inhibit both mTORC1 and mTORC2 complexes and exhibit good antiproliferative activity.
View Article and Find Full Text PDFA pharmacophore mapping approach, derived from previous experience of PIKK family enzymes, was used to identify a hit series of selective inhibitors of the mammalian target of rapamycin (mTOR). Subsequent refinement of the SAR around this hit series based on a tri-substituted triazine scaffold has led to the discovery of potent and selective inhibitors of mTOR.
View Article and Find Full Text PDFDouble asymmetric induction as a mechanistic probe indicates that, for the conjugate addition of (R)- and (S)-lithium N-benzyl-N--alpha-methylbenzylamide to (S)-3'-phenylprop-2'-enoyl-4-benzyloxazolidinone, the reactive conformation of the N-acyl oxazolidinone is the anti-s-cis form, facilitating the asymmetric synthesis of a pseudotripeptide.
View Article and Find Full Text PDF