Bolli, Martin H.; Boss, Christoph; Binkert, Christoph; Buchmann, Stephan; Bur, Daniel; Hess, Patrick; Iglarz, Marc; Meyer, Solange; Rein, Josiane; Rey, Markus; Treiber, Alexander; Clozel, Martine; Fischli, Walter; Weller, Thomas published the artcile< 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>, SDS of cas: 25999-04-6, the main research area is alkyl sulfamide pyrimidine preparation oral endothelin receptor antagonist antihypertensive.
Starting from the structure of bosentan (1), we embarked on a medicinal chem. 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 ETA with significant affinity for the ETB 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 clin. trial for pulmonary arterial hypertension.
Journal of Medicinal Chemistry published new progress about Antihypertensives. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, SDS of cas: 25999-04-6.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics