1, 3-Disubstituted-2-carboxy quinolones: highly potent and selective endothelin A receptor antagonists

JL Haesslein, I Baholet, M Fortin, A Iltis, J Khider…

Index: Haesslein, Jean-Luc; Baholet, Isabelle; Fortin, Michel; Iltis, Alain; Khider, Jean; Periers, Anne Marie; Pierre, Christine; Vevert, Jean-Paul Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 13 p. 1487 - 1490

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Citation Number: 6

Abstract

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 . ... Several peptidic as well as non-peptidic endothelin antagonists have been reported in the literature, being either ET A selective (ie, BQ 123, 8 BMS 182874, 9 A-127772, 10 ) ET B selective (BQ 788 11 ) ...