Positive inotropic agents: modelling, synthesis and SAR |
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Authors: | G A Leclerc |
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Affiliation: | Université Joseph Fourier, Faculté de Pharmacie de Grenoble, Meylan, France. |
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Abstract: | Five non steroidal cardiotonics have been studied for the search of a common pharmacophore with the aid of the SYBYL computer modelling programme. On the basis of the model thus obtained a series of pyridylquinolones have been prepared and some structure activity relationships examined. The compounds were evaluated for positive inotropic and vasodilatory activities in vitro and in vivo animal models. Several substances displayed activities higher than that of classical references, and might be beneficial in patients with congestive heart failure. |
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