New pyridazinone derivatives with vasorelaxant and platelet antiaggregatory activities.
New 6-substituted and 2,6-disubstituted pyridazinone derivatives were obtained starting from easily accessible alkyl furans by using oxidation with singlet oxygen to give 4-methoxy or 4-hydroxybutenolides, key intermediates of this synthetic strategy. The new pyridazinone derivatives have been studied as vasorelaxant and antiplatelet agents. Analysis of biological data revealed the silyl ethers (4a-i) and N,O-dibenzyl derivatives (6g-i) as the most active compounds.
Costas
Tamara
T
Departamento de Química Orgánica, Universidade de Vigo, 36310 Vigo, Spain.
Besada
Pedro
P
Piras
Alessandro
A
Acevedo
Laura
L
Yañez
Matilde
M
Orallo
Francisco
F
Laguna
Reyes
R
Terán
Carmen
C
D001792:Blood Platelets / Q000187:drug effects; D002478:Cells, Cultured; D006801:Humans; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D011724:Pyridazines / Q000494:pharmacology*; D014665:Vasodilator Agents / Q000494:pharmacology*
D010975:Platelet Aggregation Inhibitors; D011724:Pyridazines; D014665:Vasodilator Agents