2-Substituted 4-, 5- and 6-[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones and 2-Substituted 4,5-bis[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones as Potent Platelet Aggregation Inhibitors: Design, Synthesis and SAR Studies

Bert Maes; Ernesto Cano; Reyes Laguna; Nuria Fraiz; Matilde Yáñez; Guy Lemière; Tom Verhelst; Caroline Meyers; Alberto Coelho,; Abdelaziz Elmaatougi; Eddy Sotelo

doi:10.3390/ecsoc-11-01334

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2-Substituted 4-, 5- and 6-[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones and 2-Substituted 4,5-bis[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones as Potent Platelet Aggregation Inhibitors: Design, Synthesis and SAR Studies

Bert U.W. Maes

^{*

1},

Ernesto Cano

²,

Reyes Laguna

²,

Nuria Fraiz

²,

Matilde Yáñez

²,

Guy L. F. Lemière

¹,

Tom Verhelst

¹,

Caroline Meyers

¹,

Alberto Coelho,

³,

Abdelaziz Elmaatougi

⁴,

Eddy Sotelo

^{*

3, 4}

¹ Organic Synthesis, Department of Chemistry, University of Antwerp, Groenenborgerlaan 171, B-2020 Antwerpen, Belgium
² Departamento de Farmacología, Universidad de Santiago de Compostela, 15782-Santiago de Compostela, spain
³ Unidad de Química Combinatoria, Instituto de Farmacia Industrial (IFI), Spain
⁴ Departamento de Química Orgánica, Spain

Published: 30 November 2007 by MDPI in The 11th International Electronic Conference on Synthetic Organic Chemistry session Solid Phase Chemistry and Combinatorial Synthesis

https://doi.org/10.3390/ecsoc-11-01334

Abstract: A set of regioisomeric 2-substituted pyridazin-3(2H)-ones containing a 3-oxo-3- phenylprop-1-en-1-yl fragment at either position 4, 5 or 6 and 2-substituted pyridazin-3(2H)-ones containing the same fragment both at positions 4 and 5 have been synthesized and evaluated as antiplatelet agents. The study allows the identification of a new highly potent platelet aggregation inhibitor (4c) as well as the formulation of preliminary structure-activity relationships in this series.

Keywords: Platelets, pyridazin-3(2H)-ones, chalcones

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