In vitro ion channel profile and ex vivo cardiac electrophysiology properties of the R(-) and S(+) enantiomers of hydroxychloroquine.

Hydroxychloroquine (HCQ) is a derivative of the antimalaria drug chloroquine primarily prescribed for autoimmune diseases. Recent attempts to repurpose HCQ in the treatment of corona virus disease 2019 has raised concerns because of its propensity to prolong the QT-segment on the electrocardiogram, an effect associated with increased pro-arrhythmic risk. Since chirality can affect drug pharmacological properties, we have evaluated the functional effects of the R(-) and S(+) enantiomers of HCQ on six ion channels contributing to the cardiac action potential and on electrophysiological parameters of isolated Purkinje fibers.

Influence of Chirality of Lactones on the Perception of Some Typical Fruity Notes through Perceptual Interaction Phenomena in Bordeaux Dessert Wines.

Recent studies concerning the aroma of noble rot dessert wines revealed the importance of a well-known phenomenon in perfumery, the perceptual blending, to create the perception of "overripe orange" nuances. Thus, compounds associated with both oak wood aging (3-methyl-4-octanolide and eugenol) and Botrytis cinerea development under the form of noble rot (2-nonen-4-olide and γ-nonalactone) contribute to a specific aroma of great noble rot dessert wines through perceptual interaction phenomena. This synthetic perception phenomenon was established from reconstitution, addition, and omission sensory experiments, using wine extract fractions supplemented with the volatile compounds previously mentioned.

Total Synthesis of Putative 11-epi-Lyngbouilloside Aglycon.

We report here the total synthesis of 11-epi-lyngbouilloside aglycon. Our strategy features a Boeckman-type esterification followed by a RCM to form the 14-membered ring macrolactone and a late-stage side chain introduction via a Wittig olefination. Overall, the final product was obtained in 20 steps and 2% overall yield starting from commercially available 3-methyl-but-3-enol.

SAR156497, an exquisitely selective inhibitor of aurora kinases.

The Aurora family of serine/threonine kinases is essential for mitosis. Their crucial role in cell cycle regulation and aberrant expression in a broad range of malignancies have been demonstrated and have prompted intensive search for small molecule Aurora inhibitors. Indeed, over 10 of them have reached the clinic as potential anticancer therapies.