Design and synthesis of thiol containing inhibitors of matrix metalloproteinases

Article abstract of DOI:10.1016/S0960-894X(98)00716-1

A series of thiol containing derivatives was prepared. Several of these compounds were found to inhibit matrix metalloproteinases 1, 3, and 9 with selectivity towards 3 and 9. Compounds 15, 20 and 22 were administered to rats orally at 75 μmol/kg. Drug levels of compounds 20 and 22 in the plasma were found to exceed the IC₅₀ values for MMP 3 and 9 four hours after administration.