Bioorganic and Medicinal Chemistry Letters p. 2223 - 2228 (1997)
Update date:2022-08-04
Topics:
Neidhart, Werner
Breu, Volker
Burri, Kaspar
Clozel, Martine
Hirth, Georges
Klinkhammer, Uwe
Giller, Thomas
Ramuz, Henri
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 ET(A) and ET(B) receptors in the low nanomolar range and high functional antagonistic potency in vitro.
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