Author/Authors :
Amy M. Bunker، نويسنده , , Jeremy J. Edmunds، نويسنده , , Kent A. Berryman، نويسنده , , Donnelle M. Walker، نويسنده , , Michael A. Flynn، نويسنده , , Kathy M. Welch، نويسنده , , Annette M. Doherty، نويسنده ,
Abstract :
Endothelin-1 is a potent vasoconstrictor which is thought to be involved in many human disease states. We have developed a series of indole non-peptide endothelin antagonists which display nanomolar receptor affinity. The representative compound from this series is PD 159433 (22), an ETA selective antagonist with an IC50 of 2 nM. The discovery, synthesis and structure-activity relationships of this series of compounds are described.
