[Thromboxane synthetase inhibitors. I. Synthesis of some imidazolylarylmethanols and their inhibitory activity on platelet aggregation].
Several imidazolylpyridinemethanols and imidazolylbenzenemethanols were prepared and evaluated for an inhibitory activity against arachidonic acid-induced platelet aggregation. The result shows that the arylmethanol moiety is essential for the activity and may correspond to the 15-OH group of prostagrandin H2 (PGH2). Among the compounds tested, 4-[alpha-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid (XV) was found to have a potent inhibitory activity and a long duration of action. Structure-activity relationships are also discussed briefly.
Tsuruda
M
M
Mikashima
H
H
Oe
T
T
Kawasaki
K
K
Setoguchi
S
S
Naka
Y
Y
Tahara
T
T
D000818:Animals; D001095:Arachidonic Acids / Q000378:metabolism; D003864:Depression, Chemical; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D011817:Rabbits; D013329:Structure-Activity Relationship
D001095:Arachidonic Acids; D007093:Imidazoles; D010975:Platelet Aggregation Inhibitors; D011725:Pyridines