Synthesis and vasorelaxant and platelet antiaggregatory activities of a new series of 6-Halo-3-phenylcoumarins

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A series of 6-halo-3-hydroxyphenylcoumarins (resveratrol-coumarins hybrid derivatives) was synthesized in good yields by a Perkin reaction followed by hydrolysis. The new compounds were evaluated for their vasorelaxant activity in intact rat aorta rings pre-contracted with phenylephrine (PE), as well as for their inhibitory effects on platelet aggregation induced by thrombin in washed human platelets. These compounds concentration-dependently relaxed vascular smooth muscle and some of them showed a platelet antiaggregatory activity that was up to thirty times higher than that shown by trans-resveratrol and some other previously synthesized derivatives

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Quezada, E.; Delogu, G.; Picciau, C.; Santana, L.; Podda, G.; Borges, F.; García-Morales, V.; Viña, D.; Orallo, F. Synthesis and Vasorelaxant and Platelet Antiaggregatory Activities of a New Series of 6-Halo-3-phenylcoumarins. Molecules 2010, 15, 270-279

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We thank Progetto di Ricerca Scientifica 2007-Università di Cagliari and Fondazione del Banco di Sardegna, Spanish Ministerio de Sanidad y Consumo (FISS PI061537, PI061457), Xunta de Galicia (Spain; INCITE08PXIB203022PR) and Spanish Ministerio de Ciencia e Innovación (FISS PS09/00618). D. Vina acknowledges sponsorships for a tenure-track research position at the University of Santiago de Compostela from the Isidro Parga Pondal Programme of the “Dirección Xeral de Investigación e Desenvolvemento, Xunta de Galicia”. E. Quezada thanks for a postdoctoral grant from FCT (Portugal). Verónica García-Morales thanks for a predoctoral grant (FPU, AP2008-02609, Spanish Ministerio de Ciencia e Innovación). C. Picciau thanks for a predoctoral grant Master & Back-Regione Sardegna

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© 2010 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland. This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/)