Inhibition of adhesion molecule expression by N-alkylthiopyridine-benzo[ b]thiophene-2-carboxamides

The surface levels of ICAM-1 and E-selectin on activated endothelial cells can be reduced by 3-alkoxybenzo[ b]thiophene-2-carboxamides. This property is shared by several N-alkylthiopyridine substituted imides. Combining structural elements of these two diverse series lead to a new class of small molecule inhibitors of adhesion molecule expression. The surface levels of ICAM-1 and E-selectin on activated endothelial cells can be reduced by N-alkylthiopyridinebenzo[ b]thiophene-2-carboxamides. In ELISA assays compound 14 had IC 50s of 5.7 and 8.4 μM for the inhibition of ICAM-1 and E-selectin expression, respectively.