Pyridazinones with a pendant acylsulfonamide moiety as endothelin receptor antagonists

Article abstract of DOI:10.1016/S0960-894X(96)00617-8

Highly active endothelin receptor antagonists can be obtained by replacing the aryloxy group of L-749,329 by diversely substituted pyridazinone residues. The syntheses and structure-activity relationships of the new aryl-oxopyridazinyl-N-(4-arylsulfonyl)-acetamides 2 are reported. 2p with a simple dimethylpyridazinone moiety was one of the most potent compounds in vitro.