Author/Authors :
Werner Neidhart، نويسنده , , Volker Breu، نويسنده , , Kaspar Burri، نويسنده , , Martine Clozel، نويسنده , , Georges Hirth، نويسنده , , Uwe Klinkhammer، نويسنده , , Thomas Giller، نويسنده , , Henri Ramuz، نويسنده ,
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.
