- Biphenylsulfonamide endothelin receptor antagonists. Part 3: Structure-activity relationship of 4′-heterocyclic biphenylsulfonamides
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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.
- 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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p. 517 - 520
(2007/10/03)
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- Substituted biphenyl isoxazole sulfonamides
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Compounds of the formula STR1 inhibit the activity of endothelin. The symbols are defined as follows: R1, R2, R3 and R4 are each directly bonded to a ring carbon and are each independently (a) hydrogen; (b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z1, Z2 and Z3 ; (c) halo; (d) hydroxyl; (e) cyano; (f) nitro; (g) --C(O)H or --C(O)R5 ; (h) --CO2 H or --CO2 R5 ; (i) --Z4 --NR6 R7 ; (j) --Z4 --N(R10)--Z5 --NR8 R9 ; or (k) R3 and R4 together may also be alkylene or alkenylene, either of which may be substituted with Z1, Z2 and Z3, completing a 4- to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached; and the remaining symbols are as defined in the specification.
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- SUBSTITUTED BIPHENYL ISOXAZOLE SULFONAMIDES
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Compounds of the formula STR1 inhibit the activity of endothelin. The symbols are defined as follows: R 1, R 2, R 3 and R 4 are each directly bonded to a ring carbon and are each independently(a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy,
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