Vasorelaxant activity of phthalazinones and related compounds

  • Bioorg Med Chem Lett. 2006 May 15;16(10):2786-90. doi: 10.1016/j.bmcl.2006.02.003.
Esther del Olmo  1 ,  Bianca Barboza ,  Maria Inés Ybarra ,  José Luis López-Pérez ,  Rosalía Carrón ,  Maria Angeles Sevilla ,  Cinthia Boselli ,  Arturo San Feliciano
Affiliations
  • 1. Departamento de Química Farmacéutica, CISET, Facultad de Farmacia, Universidad de Salamanca, 37007 Salamanca, Spain. [email protected]
PMID: 16513345 DOI: 10.1016/j.bmcl.2006.02.003
Abstract

Several series of dihydrostilbenamide, imidazo[2,1-a]isoindole, pyrimido[2,1-a]isoindole and phthalazinone derivatives were obtained and their vasorelaxant activity was measured on isolated rat aorta rings pre-contracted with phenylephrine (10(-5)M). Some phthalazinones attained, practically, the total relaxation of the organ at micromolar concentrations. For the most potent compound 9h (EC(50)=0.43microM) the affinities for alpha(1A), alpha(1B) and alpha(1D) adrenergic sub-receptors were determined.

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