Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from bosentan

Bioorganic & Medicinal Chemistry Letters
1997.0

Abstract

Implementation of a pyridylcarbamoyl group and an isopropylpyridylsulfonamide substituent as key components in the scaffold of Bosentan resulted in the identification of the potent orally active endothelin receptor antagonist Ro 48-5695. It shows affinities for ETA and ETB receptors in the low nanomolar range and high functional antagonistic potency in vitro.

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