Synthesis and structure-activity relationships of 9-substituted acridines as endothelin-A receptor antagonists

X.‐M. Cheng,Chitase Lee,Sylvester Klutchko,T. Winters,Elwood E. Reynolds,Kathy M. Welch,Michael A. Flynn,Annette Marian Doherty

Synthesis and structure-activity relationships of 9-substituted acridines as endothelin-A receptor antagonists

1996

X.‐M. Cheng
Chitase Lee
Sylvester Klutchko
T. Winters
Elwood E. Reynolds
Kathy M. Welch
Michael A. Flynn
Annette Marian Doherty

Abstract Screening of a compound library against endothelin receptors (ET A and ET B ) revealed PD 102566 (compound 1 ) as an ET A selective antagonist. Synthesis and structure-activity relationships (SAR) of a series of analogs are described.

Keywords:

Antagonist
Endothelin A Receptor Antagonists
Acridine derivatives
Stereochemistry
Structure–activity relationship
Biochemistry
Endothelin receptor
Chemistry
selective antagonist

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