1,3-Disubstituted-2-carboxy quinolones: highly potent and selective endothelin A receptor antagonists.
The design, synthesis, and in vitro biological activity of a series of 2-carboxy quinolone antagonists selective for the endothelin A receptor are presented. Introduction of a second acid group in position 3 of the quinolone ring increases dramatically the selectivity for ET(A).
Haesslein
J L
JL
Medicinal Chemistry, Hoechst Marion Roussel, Romainville, France. jean-luc.haesslein@aventis.com
Baholet
I
I
Fortin
M
M
Iltis
A
A
Khider
J
J
Periers
A M
AM
Pierre
C
C
Vevert
J P
JP
D000818:Animals; D001681:Biological Assay; D003500:Cyclization; D015195:Drug Design; D065128:Endothelin Receptor Antagonists; D005260:Female; D006801:Humans; D008297:Male; D051379:Mice; D015394:Molecular Structure; D015363:Quinolones / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D044022:Receptor, Endothelin A; D017466:Receptors, Endothelin / Q000378:metabolism; D013329:Structure-Activity Relationship
D065128:Endothelin Receptor Antagonists; D015363:Quinolones; D044022:Receptor, Endothelin A; D017466:Receptors, Endothelin