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

Resultado de la investigación: Review article

9 Citas (Scopus)

Resumen

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.

Idioma originalEnglish
Páginas (desde-hasta)547-570
Número de páginas24
PublicaciónEuropean Journal of Medicinal Chemistry
Volumen32
N.º7-8
DOI
EstadoPublished - 1 ene 1997

Huella dactilar

4-Quinolones
Substitution reactions
Pharmacology
leukotriene D4 receptor
pranlukast
In Vitro Techniques

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Citar esto

Griera, R. ; Armengol, M. ; Reyes, A. ; Alvarez, M. ; Palomer, A. ; Cabré, F. ; Pascual, J. ; García, M. L. ; Mauleón, D. / Synthesis and pharmacological evaluation of new cysLT1 receptor antagonists. En: European Journal of Medicinal Chemistry. 1997 ; Vol. 32, N.º 7-8. pp. 547-570.
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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.",
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author = "R. Griera and M. Armengol and A. Reyes and M. Alvarez and A. Palomer and F. Cabr{\'e} and J. Pascual and Garc{\'i}a, {M. L.} and D. Maule{\'o}n",
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Griera, R, Armengol, M, Reyes, A, Alvarez, M, Palomer, A, Cabré, F, Pascual, J, García, ML & Mauleón, D 1997, 'Synthesis and pharmacological evaluation of new cysLT1 receptor antagonists', European Journal of Medicinal Chemistry, vol. 32, n.º 7-8, pp. 547-570. https://doi.org/10.1016/S0223-5234(97)83282-5

Synthesis and pharmacological evaluation of new cysLT1 receptor antagonists. / Griera, R.; Armengol, M.; Reyes, A.; Alvarez, M.; Palomer, A.; Cabré, F.; Pascual, J.; García, M. L.; Mauleón, D.

En: European Journal of Medicinal Chemistry, Vol. 32, N.º 7-8, 01.01.1997, p. 547-570.

Resultado de la investigación: Review article

TY - JOUR

T1 - Synthesis and pharmacological evaluation of new cysLT1 receptor antagonists

AU - Griera, R.

AU - Armengol, M.

AU - Reyes, A.

AU - Alvarez, M.

AU - Palomer, A.

AU - Cabré, F.

AU - Pascual, J.

AU - García, M. L.

AU - Mauleón, D.

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AB - 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.

KW - 4-quinolons

KW - Acylsulfonamide

KW - Antagonist

KW - Leukotriene D

KW - Molecular modelling

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