2. Academic Validation
  3. The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists

The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists

  • Bioorg Med Chem Lett. 2003 Mar 10;13(5):955-9. doi: 10.1016/s0960-894x(02)01084-3.
Martin H Bolli 1,  Christoph Boss,  Martine Clozel,  Walter Fischli,  Patrick Hess,  Thomas Weller
Affiliations

Affiliation

  • 1 Drug Discovery Chemistry and Preclinical Research, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, CH-4123 Allschwil/BL, Switzerland. martin.bolli@actelion.com
PMID: 12617929 DOI: 10.1016/s0960-894x(02)01084-3
Abstract

A series of compounds structurally related to bosentan 1 featuring an unsaturated side chain at position 6 of the core pyrimidine have been studied for their potential to block the ET(A) and ET(B) receptor. Incorporation of a 2-butyne-1,4-diol linker bearing a pyridyl carbamoyl moiety led to in vitro highly potent Endothelin Receptor antagonists (e.g., 70 and 75). The propargyl derivative 26 significantly reduced blood pressure in in vivo model studies with hypertensive salt-sensitive Dahl rats.

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