Pyridazines part 41: synthesis, antiplatelet activity and SAR of 2,4,6-substituted 5-(3-oxo-3-phenylprop-1-en-1-yl)- or 5-(3-phenylprop-2-enoyl)pyridazin-3(2H)-ones

Abel Crespo; Caroline Meyers; Alberto Coelho; Matilde Yáñez; Nuria Fraiz; Eddy Sotelo; Bert U W Maes; Reyes Laguna; Ernesto Cano; Guy L F Lemière; Enrique Raviña

doi:10.1016/j.bmcl.2005.10.073

Pyridazines part 41: synthesis, antiplatelet activity and SAR of 2,4,6-substituted 5-(3-oxo-3-phenylprop-1-en-1-yl)- or 5-(3-phenylprop-2-enoyl)pyridazin-3(2H)-ones

Bioorg Med Chem Lett. 2006 Feb 15;16(4):1080-3. doi: 10.1016/j.bmcl.2005.10.073. Epub 2005 Nov 14.

Authors

Abel Crespo¹, Caroline Meyers, Alberto Coelho, Matilde Yáñez, Nuria Fraiz, Eddy Sotelo, Bert U W Maes, Reyes Laguna, Ernesto Cano, Guy L F Lemière, Enrique Raviña

Affiliation

¹ Departamento de Química Orgánica, Laboratorio de Química Farmacéutica, Universidad de Santiago de Compostela, 15782-Santiago de Compostela, España, Spain.

PMID: 16290144
DOI: 10.1016/j.bmcl.2005.10.073

Abstract

As part of the optimization process of the lead compound I a focussed library of diversely substituted pyridazin-3(2H)-ones containing a 3-oxo-3-phenylprop-1-en-1-yl or 3-phenylprop-2-enoyl fragment at position 5 has been obtained and evaluated as antiplatelet agents. The structural modification at positions 2, 6 and 4 of the heterocyclic moiety allowed us to obtain preliminary information on the structure-activity relationship in this family.

MeSH terms

Molecular Structure
Platelet Aggregation / drug effects*
Platelet Aggregation Inhibitors / chemical synthesis*
Platelet Aggregation Inhibitors / chemistry
Platelet Aggregation Inhibitors / pharmacology
Pyridazines / chemical synthesis*
Pyridazines / chemistry
Pyridazines / pharmacology*
Stereoisomerism
Structure-Activity Relationship

Substances

Platelet Aggregation Inhibitors
Pyridazines