181133-18-6Relevant articles and documents
Biphenylsulfonamide endothelin receptor antagonists. Part 3: Structure-activity relationship of 4′-heterocyclic biphenylsulfonamides
Murugesan, Natesan,Gu, Zhengxiang,Stein, Philip D.,Spergel, Steven,Bisaha, Sharon,Liu, Eddie C.-K.,Zhang, Rongan,Webb, Maria L.,Moreland, Suzanne,Barrish, Joel C.
, p. 517 - 520 (2007/10/03)
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.