Isoindolines: a new series of potent and selective endothelin-A receptor antagonists.
1,3-Disubstituted isoindolines have been discovered as a new class of potent functional ET(A) selective receptor antagonists through pharmacophore analysis of existing nonpeptide endothelin antagonists. The structure-activity relationships for both the trans and the cis series of isoindolines are discussed.
Kukkola
P J
PJ
Metabolic and Cardiovascular Diseases, Novartis Institute for Biomedical Research, 07901, Summit NJ, USA. paivi.kukkola@pharma.novartis.com
Bilci
N A
NA
Ikler
T
T
Savage
P
P
Shetty
S S
SS
DelGrande
D
D
Jeng
A Y
AY
D065128:Endothelin Receptor Antagonists; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D044022:Receptor, Endothelin A; D017466:Receptors, Endothelin / Q000737:chemistry
D065128:Endothelin Receptor Antagonists; D007211:Indoles; D044022:Receptor, Endothelin A; D017466:Receptors, Endothelin