Novel inhibitors of prolyl 4-hydroxylase

摘要: A series of 5-acyl sulfonamides derived from pyridine-2,5-dicarboxylic acid (15) has been prepared and several members this have shown to be more potent, in vitro, as inhibitors prolyl 4-hydroxylase than 15. Several chain-extended pyridinedicarboxylic acids also potent 4-hydroxylase. The structure-activity both these is discussed. results indicate that the 5-carboxylic binding site, enzyme, can accept a carboxylic or an acyl sulfonamide equally well. This indicates much greater degree freedom distal site predicted by current theoretical model active site.