Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from Bosentan

DOI: 10.1016/S0960-894X(97)00400-9

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 2223 - 2228 (1997)

Update date:2022-08-04

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Authors:

Neidhart, Werner

Breu, Volker

Burri, Kaspar

Clozel, Martine

Hirth, Georges

Klinkhammer, Uwe

Giller, Thomas

Ramuz, Henri

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Article abstract of DOI:10.1016/S0960-894X(97)00400-9

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.

Full text of DOI:10.1016/S0960-894X(97)00400-9

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