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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
* 1 , 2 , 2 , 2 , 2 , 1 , 1 , 1 , 3 , 4 , * 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

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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