Author/Authors :
Natesan Murugesan، نويسنده , , Zhengxiang Gu، نويسنده , , Philip D. Stein، نويسنده , , Steven Spergel، نويسنده , , Sharon Bisaha، نويسنده , , Eddie C. -K. Liu، نويسنده , , Rongan Zhang، نويسنده , , Maria L. Webb، نويسنده , , Suzanne Moreland، نويسنده , , Joel C. Barrish، نويسنده ,
Abstract :
A number of 4′-heterocyclic biphenylsulfonamide derivatives, formally derived from BMS-193884 (1) by replacing the oxazole ring with other heterocyclic rings, are potent and selective endothelin A (ETA) receptor antagonists. Among the analogues examined, the pyrimidine derivative 18 is the most potent (Ki=0.9 nM) and selective for the ETA receptor, approximately equivalent to 1.