Design and Synthesis of E-Selectin Antagonists

摘要

Selectin-mediated recruitment of leukocytes plays a crucial role in a number of diseases and pathological situations. For example in inflammation, reperfusion injury, rheumatoid arthritis and respiratory diseases. Substantial research efforts are directed toward development of carbohydrate-derived drugs that interfere with the inflammatory response by blocking the selection binding site. This article describes two approaches for the improvement of the inhibitory potency of the lead structure sialyl Lewis~x (sLe~x). One approach is based on the preorganization of mimics in their bioactive conformation to reduce entropic costs.