Inhibitors of MMP-1: An examination of P1' Cα gem-disubstitution in the N-carboxylalkylamine and glutaramide carboxylate series

Article abstract of DOI:10.1016/0960-894X(96)00304-6

Modification of the N-carboxyalkylamine 3 by independent replacement of the P₁' NH group for CH₂ and introduction of P₁' gem-cyclohexyl substitution affords compounds 5 and 6a which retain appreciable activity against MMP-1 (IC₅₀s = 0.023 μM and 0.09 μM, respectively). The glutaramide 7a which incorporates both these structural changes also retains potent activity (IC₅₀ = 0.038 μM).