Synthesis and pharmacological evaluation of new cysLT1 receptor antagonists

R. Griera, M. Armengol, A. Reyes, M. Alvarez, A. Palomer, F. Cabré, J. Pascual, M. L. García, D. Mauleón

Research output: Contribution to journalArticlepeer-review

9 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)547-570
Number of pages24
JournalEuropean Journal of Medicinal Chemistry
Volume32
Issue number7-8
DOIs
Publication statusPublished - 1997

Keywords

  • 4-quinolons
  • Acylsulfonamide
  • Antagonist
  • Leukotriene D
  • Molecular modelling

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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