Title of article
Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from bosentan
Author/Authors
Werner Neidhart، نويسنده , , Volker Breu، نويسنده , , Kaspar Burri، نويسنده , , Martine Clozel، نويسنده , , Georges Hirth، نويسنده , , Uwe Klinkhammer، نويسنده , , Thomas Giller، نويسنده , , Henri Ramuz، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 1997
Pages
6
From page
2223
To page
2228
Abstract
Implementation of a pyridylcarbamoyl group and an isopropylpyridylsulfonamide substituent as key components in the scaffold of Bosentan resulted in the identification of the potent orally active endothelin receptor antagonist Ro 48-5695. It shows affinities for ETA and ETB receptors in the low nanomolar range and high functional antagonistic potency in vitro.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
1997
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
788936
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