Sialyl Lewis glycomimetics bearing an extended anionic chain targeting E- and P- selectin binding sites.

Neutrophil binding to vascular P- and E-selectin is the rate-limiting step in the recruitment of immune cells to sites of inflammation. Many diseases, including sickle cell anemia, post-myocardial infarction reperfusion injury, and acute respiratory distress syndrome are characterized by dysregulated inflammation. We have recently reported sialyl Lewis analogues as potent antagonists of P- and E-selectin and demonstrated their in vivo immunosuppressive activity.

Intramolecular sp(3) Functionalization of Cyclopropyl α-Amino Acid-Derived Benzamides.

Intramolecular Pd-catalyzed functionalization of cyclopropyl α-amino acid-derived benzamides proceeds without silver or pivalate additives. Both electronically and sterically diverse ethyl 1,2,3,4-tetrahydroisoquinolone-3-carboxylates were accessible in good to excellent yields.