Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists

Bioorganic & Medicinal Chemistry Letters
1996.0

Abstract

Replacement of the 4-methyl group in a series of N-(3,4-dimethylisoxazolyl)benzenesulfonamide endothdin antagonists with a bromine or chlorine atom resulted in a three- to ten-fold increase in the binding affinity for both the ETA and ETB receptors. This potentiation in activities was also observed for naphthalene and biphenylsulfonamide endothelin antagonists.

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