bq-123 and macitentan
bq-123 has been researched along with macitentan* in 1 studies
Other Studies
1 other study(ies) available for bq-123 and macitentan
| Article | Year |
|---|---|
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.
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 properties and high in vivo efficacy in hypertensive Dahl salt-sensitive rats. Compound 17 successfully completed a long-term phase III clinical trial for pulmonary arterial hypertension. Topics: Administration, Oral; Animals; Antihypertensive Agents; CHO Cells; Cricetinae; Cricetulus; Drug Discovery; Endothelin A Receptor Antagonists; Endothelin B Receptor Antagonists; Pyrimidines; Rats; Rats, Inbred Dahl; Sulfonamides | 2012 |