European Journal of Medicinal Chemistry p. 547 - 570 (1997)
Update date:2022-08-04
Topics:
Griera
Armengol
Reyes
Alvarez
Palomer
Cabre
Pascual
Garcia
Mauleon
This paper describes the synthesis and pharmacological evaluation of three series of compounds 4a-b, 13a-k and 19, structurally related to the known potent cysLT1 receptor antagonists RG-12553, IC1-204219 and ONO-1078, respectively. The common structural feature of these new series is the presence of a 4-quinolone nucleus acting as a template for substitution of the aromatic nucleus present in the prototype antagonists. We describe the evolution of these series leading to antagonists with potency at nanomolar concentrations in vitro.
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