The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist.

@article{Bolli2012TheDO,
  title={The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist.},
  author={Martin H. Bolli and Christoph Boss and Christoph Binkert and Stephan Buchmann and Daniel Bur and Patrick J. Hess and Marc Iglarz and Solange Meyer and Josiane Rein and Markus Rey and Alexander Treiber and Martine Clozel and Walter Fischli and Thomas Weller},
  journal={Journal of medicinal chemistry},
  year={2012},
  volume={55 17},
  pages={7849-61}
}
Starting from the structure of bosentan (1), we embarked on a medicinal chemistry program aiming at the identification of novel potent dual endothelin receptor antagonists with high oral efficacy. This led to the discovery of a novel series of alkyl sulfamide substituted pyrimidines. Among these, compound 17 (macitentan, ACT-064992) emerged as particularly interesting as it is a potent inhibitor of ET(A) with significant affinity for the ET(B) receptor and shows excellent pharmacokinetic… CONTINUE READING
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