A new group of 5,5-diarylhydantoin derivatives bearing a methylsulfonyl COX-2 pharmacophore at the para position of the C-5 phenyl ring were designed and synthesized as selective COX-2 inhibitors. In vitro COX-1/COX-2 inhibition structure-activity relationships identified 5-[4-(methylsulfonyl)phenyl]-5-phenyl-hydantoin (4) as a highly potent and selective COX-2 inhibitor (COX-2 IC(50) = 0.077 μ...

Leishmaniasis represents a serious threat to the health as one of the most important neglected tropical diseases as designated by the World Health Organization. The disease is endemic in 82 countries, among them Tunisia is an indigenous area for cutaneous Leishmaniasis. In a previous work, two tritepenic acids namely oleanolic and maslinic acids have been isolated from olive leaf extract. In th...

The paper presents a novel method for compressing large database workloads for purpose of autonomic, continuous index selection. The compressed workload contains a small subset of representative queries from the original workload. A single pass clustering algorithm with a simple and elegant selectivity based query distance metric guarantees low memory and time complexity. Experiments on two rea...

This poster describes three static SPARQL optimization approaches for in-memory RDF graphs: (1) a selectivity estimation index (SEI) for single query triple patterns; (2) a query pattern index (QPI) for joined triple patterns; and (3) a hybrid optimization approach that combines both indexes. Using the Lehigh University Benchmark (LUBM), we show that the hybrid approach outperforms other SPARQL...

A quinazolinedione-derived screening hit 2 was discovered with cellular antiviral activity against respiratory syncytial virus (CPE EC50 = 2.1 μM), moderate efficacy in reducing viral progeny (4.2 log at 10 μM), and marginal cytotoxic liability (selectivity index, SI ∼ 24). Scaffold optimization delivered analogs with improved potency and selectivity profiles. Most notable were compounds 15 and...

Primary visual cortex (V1) provides crucial insights into the selectivity and emergence of specific output features such as orientation tuning. Tuning and selectivity of cortical neurons in mouse visual cortex is not equivocally resolved so far. While many in-vivo experimental studies found inhibitory neurons of all subtypes to be broadly tuned for orientation other studies report inhibitory ne...

The impressive performance and plasticity of convolutional neural networks to solve different vision problems are shadowed by their black-box nature and its consequent lack of full understanding. To reduce this gap we propose to describe the activity of individual neurons by quantifying their inherent selectivity to specific properties. Our approach is based on the definition of feature selecti...

Conditions for the equilibrium binding to opioid receptor of [3H]sufentanil (mu selective), [3H][D-Pen2,D-Pen5]enkephalin (delta selective), and [3H]U69,593 (kappa selective) were established in membranes from rat brain cerebrum, monkey cortex, or guinea pig cerebellum. The selectivity index of various opioid alkaloids and peptides in binding to the mu, delta, or kappa opioid receptors was expr...

Semantic web search engine Falcons support keyword based search for linked objects by using comprehensive virtual document which it creates for each object. In our work we are suggesting idea of using Selectivity Estimation of triple patterns for ranking of resulting objects and generating snippet for the keyword query for Falcons Semantic web search engine. Selectivity of a triple pattern is t...