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Pyridazinones with a pendant acylsulfonamide moiety as endothelin receptor antagonists

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.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N305 – PubChem