DISCOVERY OF RO-48-5695 - A POTENT MIXED ENDOTHELIN RECEPTOR ANTAGONIST OPTIMIZED FROM BOSENTAN

Authors
NEIDHART W BREU V BURRI K CLOZEL M HIRTH G KLINKHAMMER U GILLER T RAMUZ H
Citation
W. Neidhart et al., DISCOVERY OF RO-48-5695 - A POTENT MIXED ENDOTHELIN RECEPTOR ANTAGONIST OPTIMIZED FROM BOSENTAN, Bioorganic & medicinal chemistry letters, 7(17), 1997, pp. 2223-2228
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
17
Year of publication
1997
Pages
2223 - 2228
Database
ISI
SICI code
0960-894X(1997)7:17<2223:DOR-AP>2.0.ZU;2-L
Abstract
Implementation of a pyridylcarbamoyl group and an isopropylpyridylsulf onamide substituent as key components in the scaffold of Bosentan resu lted in the identification of the potent orally active endothelin rece ptor antagonist Ro 48-5695. It shows affinities for ETA and ETB recept ors in the low nanomolar range and high functional antagonistic potenc y in vitro. (C) 1997 Elsevier Science Ltd.