Vasorelaxant activity of phthalazinones and related compounds.

Bioorg Med Chem Lett

Departamento de Química Farmacéutica, CISET, Facultad de Farmacia, Universidad de Salamanca, 37007 Salamanca, Spain.

Published: May 2006

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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http://dx.doi.org/10.1016/j.bmcl.2006.02.003DOI Listing

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