申请人:The Scripps Research Institute
公开号:US05830871A1
公开(公告)日:1998-11-03
Inhibitors of E-, P- and L-selectin binding are synthesized by an aldol addition reaction between a glycoside aldehyde precursor and dihydroxyacetone phosphate or a derivative thereof. The addition reaction is catalyzed by aldolase. The inhibitors exhibit an activity comparable to sialyl Lewis X with respect to the E-selectin binding assay and high activities in the P- and L-selectin binding assays. The inhibitors are employable for blocking neutrophil inflamatory conditions.
E-, P- 和 L- 选择素结合的抑制剂是通过糖苷缩醛前体和二羟基乙酮磷酸盐或其衍生物之间的醛缩反应合成的。醛缩反应由醛缩酶催化。这些抑制剂在 E- 选择素结合试验中表现出与唾液酸 Lewis X 相当的活性,并在 P- 和 L- 选择素结合试验中表现出高活性。这些抑制剂可用于阻止中性粒细胞炎症情况。