Hydropersulfide (RSSH)-Mediated Hydrothiolation of Alkenes.

A hydropersulfide-mediated hydrothiolation reaction of alkenes has been developed for C-S bond formation with Markovnikov selectivity. This new approach is a transition-metal-, additive-, and solvent-free reaction under mild conditions. The reaction is postulated to proceed by an ionic mechanism with the release of elemental sulfur based on our control experiments and density functional theory calculations.

Toward Dose Prediction at Point of Design.

Human dose prediction (HDP) is a useful tool for compound optimization in preclinical drug discovery. We describe here our exclusively in silico HDP strategy to triage compound designs for synthesis and experimental profiling. Our goal is a model that provides a preliminary estimate of the dose for a given exposure target based on chemical structure.

Synthesis of unsymmetrical phosphorus disulfides.

A sulfur-mediated umpolung strategy employing -thiosuccinimides and (EtO)P(O)SH has been developed to synthesize unsymmetrical organophosphorus disulfides (P(O)-S-S motif). A pronucleophile (EtO)P(O)SH, Brønsted acid and phosphorothioate nucleophile, converts -thiosuccinimides into unsymmetrical phosphorus disulfides. This protocol achieves catalyst- and additive-free reaction conditions, uses a renewable solvent (EtOH), and avoids harsh reagents.

Acyl-CoA synthetase 6 controls rod photoreceptor function and survival by shaping the phospholipid composition of retinal membranes.

The retina is light-sensitive neuronal tissue in the back of the eye. The phospholipid composition of the retina is unique and highly enriched in polyunsaturated fatty acids, including docosahexaenoic fatty acid (DHA). While it is generally accepted that a high DHA content is important for vision, surprisingly little is known about the mechanisms of DHA enrichment in the retina.