Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides |
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| Authors: | 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 |
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| Institution: | Department of Chemistry, Cardiovascular Agents, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-5400, USA. natesan.murugesan@bms.com |
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| 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 (ET(A)) receptor antagonists. Among the analogues examined, the pyrimidine derivative 18 is the most potent (K(i)=0.9 nM) and selective for the ET(A) receptor, approximately equivalent to 1. |
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