N-Methyl-2-[4-(2-methylpropyl)phenyl]-3-(3- methoxy-5-methylpyrazin-2-ylsulfamoyl)benzamide; one of a class of novel benzenesulphonamides which are orally-active, ET(A)-seIective endothelin antagonists

DOI: 10.1016/S0960-894X(97)00228-X

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1399 - 1402 (1997)

Update date:2022-08-05

Topics:

Authors:

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.

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Article abstract of DOI:10.1016/S0960-894X(97)00228-X

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.

Full text of DOI:10.1016/S0960-894X(97)00228-X

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