Synthesis and vasorelaxant and antiplatelet activities of a new series of (4-Benzylphthalazin-1-ylamino)alcohol derivatives

A new series of phthalazine derivatives was synthesized by reaction of phthalic anhydride and different substituted phenylacetic acids to yield the benzyliden-3H-isobenzofuran-1-one intermediates 2a – d . Treatment of them with hydrazine afforded 4-benzyl-2H-phthalazin-1-one derivatives 3a – d , whi...

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Bibliographic Details
Published in:Medicinal chemistry research Vol. 26; no. 8; pp. 1682 - 1688
Main Authors: Munín, Javier, Quezada, Elías, Campos-Toimil, Manuel, Cano, Ernesto, Uriarte, Eugenio, Viña, Dolores
Format: Journal Article
Language:English
Published: New York Springer US 01-08-2017
Springer Nature B.V
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Summary:A new series of phthalazine derivatives was synthesized by reaction of phthalic anhydride and different substituted phenylacetic acids to yield the benzyliden-3H-isobenzofuran-1-one intermediates 2a – d . Treatment of them with hydrazine afforded 4-benzyl-2H-phthalazin-1-one derivatives 3a – d , which were substituted with the corresponding aminoalkylalcohol to obtain the (4-benzylphthalazin-1-ylamino)alcohol derivatives 4a – h . In general, these phthalazine derivatives relaxed the contractions produced by phenylephrine both in intact or endothelium-denuded aortic rings. In addition, platelet aggregation induced by thrombin was also inhibited by compounds 4c and 4g .
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-017-1879-9