From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective

Bioorganic and Medicinal Chemistry Letters

Volumn 26, Issue 15, 2016, Pages 3381-3394

  Boss, Christoph ^a   Bolli, Martin H ^a   Gatfield, John ^a  

^a ACTELION PHARMACEUTICALS LTD   (Switzerland)

Author keywords

Endothelin; Endothelin receptor antagonists (ERA); G protein coupled receptor (GPCR); Macitentan; Pulmonary arterial hypertension (PAH); Pyrimidine; Sulfamide

Indexed keywords

AMBRISENTAN; ATRASENTAN; AVOSENTAN; BMS 193884; BOSENTAN; CLAZOSENTAN; DARUSENTAN; ENRASENTAN; FANDOSENTAN; MACITENTAN; SITAXSENTAN; TEZOSENTAN; ZIBOTENTAN; ENDOTHELIN RECEPTOR; PYRIMIDINE DERIVATIVE; SULFONAMIDE;

ARTERIAL PRESSURE; BINDING AFFINITY; CARDIOVASCULAR DISEASE; CHRONIC DISEASE; DOSE RESPONSE; DRUG EFFICACY; HIGH THROUGHPUT SCREENING; HUMAN; IC50; IN VITRO STUDY; IN VIVO STUDY; LONG TERM CARE; NONHUMAN; PULMONARY HYPERTENSION; REVIEW; STRUCTURE ACTIVITY RELATION; CHEMICAL STRUCTURE; CHEMISTRY; MEDICINAL CHEMISTRY; METABOLISM;

CHEMISTRY, PHARMACEUTICAL; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MOLECULAR STRUCTURE; PYRIMIDINES; RECEPTORS, ENDOTHELIN; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

EID: 84978420809     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2016.06.014     Document Type: Review

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