(3-METHOXY-5-METHYLPYRAZIN-2-YLSULFAMOYL)BENZAMIDE - ONE OF A CLASS OF NOVEL BENZENESULFONAMIDES WHICH ARE ORALLY-ACTIVE, ETA-SELECTIVE ENDOTHELIN ANTAGONISTS

Authors
MORTLOCK AA BATH C BUTLIN RJ HEYS C HUNT SJ REID AC SUMNER NF TANG EK WHITING E WILSON C WRIGHT ND
Citation
Aa. Mortlock et al., (3-METHOXY-5-METHYLPYRAZIN-2-YLSULFAMOYL)BENZAMIDE - ONE OF A CLASS OF NOVEL BENZENESULFONAMIDES WHICH ARE ORALLY-ACTIVE, ETA-SELECTIVE ENDOTHELIN ANTAGONISTS, Bioorganic & medicinal chemistry letters, 7(11), 1997, pp. 1399-1402
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
11
Year of publication
1997
Pages
1399 - 1402
Database
ISI
SICI code
0960-894X(1997)7:11<1399:(-OOAC>2.0.ZU;2-X
Abstract
A series of novel sulphonamides have been discovered which show high a ffinity and selectivity for the endothelin ETA receptor. 3-methoxy-5-m ethylpyrazin-2-yl-sulfamoyl)benzamide (18) is the most widely investig ated compound and is a potent antagonist in vivo when dosed either i.v . or orally, and has prolonged oral duration of action. (C) 1997 Elsev ier Science Ltd.