Bioorganic and Medicinal Chemistry Letters p. 1399 - 1402 (1997)
Update date:2022-08-05
Topics:
Mortlock, Andrew A.
Bath, Colin
Butlin, Roger J.
Heys, Christine
Hunt, Sarah J.
Reid, Alan C.
Sumner, Neil F.
Tang, Eric K.
Whiting, Elaine
Wilson, Campbell
Wright, Nicola D.
A series of novel sulphonamides have been discovered which show high affinity and selectivity for the endothelin ET(A) receptor. N-Methyl-2-[4-(2-methylpropyl)phenyl]-3-(-3-methoxy-5-methylpyrazin-2 -ylsulfamoyl)benzamide (18) is the most widely investigated compound and is a potent antagonist in vivo when dosed either i.v. or orally, and has prolonged oral duration of action.
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