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.
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).
Organic Synthesis, Department of Chemistry, University of Antwerp, Groenenborgerlaan 171, B-2020 Antwerpen, Belgium.
Caroline
C
Meyers
Matilde
M
Yáñez
Abdelaziz
A
Elmaatougi
Tom
T
Verhelst
Alberto
A
Coelho
Nuria
N
Fraiz
Guy L F
GL
Lemière
Xerardo
X
García-Mera
Reyes
R
Laguna
Ernesto
E
Cano
Bert U W
BU
Maes
Eddy
E
Sotelo
D015195:Drug Design; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011724:Pyridazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D010975:Platelet Aggregation Inhibitors; D011724:Pyridazines