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.
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.
Crespo
Abel
A
Departamento de Química Orgánica, Laboratorio de Química Farmacéutica, Universidad de Santiago de Compostela, 15782-Santiago de Compostela, España, Spain.
Meyers
Caroline
C
Coelho
Alberto
A
Yáñez
Matilde
M
Fraiz
Nuria
N
Sotelo
Eddy
E
Maes
Bert U W
BU
Laguna
Reyes
R
Cano
Ernesto
E
Lemière
Guy L F
GL
Raviña
Enrique
E
D015394:Molecular Structure; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011724:Pyridazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D010975:Platelet Aggregation Inhibitors; D011724:Pyridazines