13552-93-7Relevant academic research and scientific papers
Discovery of a new class of potent MMP inhibitors by structure-based optimization of the arylsulfonamide scaffold
Mori, Mattia,Massaro, Assunta,Calderone, Vito,Fragai, Marco,Luchinat, Claudio,Mordini, Alessandro
, p. 565 - 569 (2013/07/26)
A new class of potent matrix metalloproteinase (MMP) inhibitors designed by structure-based optimization of the well-known arylsulfonamide scaffold is presented. Molecules show an ethylene linker connecting the sulfonamide group with the P1' aromatic portion and a D-proline residue bearing the zinc-binding group. The affinity improvement provided by these modifications led us to discover a nanomolar MMP inhibitor bearing a carboxylate moiety as zinc-binding group, which might be a promising lead molecule. Notably, a significant selectivity for MMP-8, MMP-12, and MMP-13 was observed with respect to MMP-1 and MMP-7.
N-Sulfonyl homoserine lactones as antagonists of bacterial quorum sensing
Castang, Sandra,Chantegrel, Bernard,Deshayes, Christian,Dolmazon, René,Gouet, Patrice,Haser, Richard,Reverchon, Sylvie,Nasser, William,Hugouvieux-Cotte-Pattat, Nicole,Doutheau, Alain
, p. 5145 - 5149 (2007/10/03)
A series of 11 N-sulfonyl homoserine lactones has been synthesised. Some of them were found to competitively inhibit the action of 3-oxohexanoyl-L- homoserine lactone, the natural inducer of bioluminescence in the bacterium Vibrio fischeri. Molecular modeling suggests a possible explanation based on the prevention of structural rearrangements necessary for the formation of the active dimer of LuxR.
