Title of article :
β-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: Part 1. Design, synthesis, and lead identification
Author/Authors :
Shyh-Ming Yang، نويسنده , , Robert H. Scannevin، نويسنده , , Bingbing Wang، نويسنده , , Sharon L. Burke، نويسنده , , Lawrence J. Wilson، نويسنده , , Prabha Karnachi، نويسنده , , Kenneth J. Rhodes، نويسنده , , Bharat Lagu، نويسنده , , William V. Murray، نويسنده ,
Abstract :
A new series of β-N-biaryl ether sulfonamide hydroxamates as novel gelatinase inhibitors is described. These compounds exhibit good potency for MMP-2 and MMP-9 without inhibiting MMP-1. The structure–activity relationships (SAR) reveal the biaryl ether type P1′ moiety together with methanesulfonamide is the optimal combination that provides inhibitory activity of MMP-9 in the single-digit nanomolar range.
Keywords :
matrix metalloproteinase , MMP inhibitor , Gelatinase , Hydroxamate
