Pyridazines. XIII. Synthesis of 6-aryl-5-oxygenated substituted-3(2H)- pyridazinones and evaluation as platelet aggregation inhibitors

DOI: 10.1248/cpb.45.1151

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 1151 - 1155 (1997)

Update date:2022-08-03

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Authors:

Laguna, Reyes

Rodriguez-Linares, Belen

Cano, Ernesto

Estevez, Isabel

Ravina, Enrique

Sotelo, Eddy

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Article abstract of DOI:10.1248/cpb.45.1151

Several 6-aryl-5-oxygenated substituted pyridazinones have been synthesized and evaluated in vitro for inhibition of platelet aggregation induced by adenosine 5'-diphosphate (ADP), thrombin and collagen. All the tested compounds (except 8 and 9) inhibited platelet aggregation in a dose- dependent manner. The IC₅₀ of the most active substance compound 2b, was around 60 μM against ADP and collagen as inducers. The inhibition of platelet aggregation caused by test compounds was dependent on the level of oxidation of the function at the 5-position, with the order of IC₅₀ values being R-OH (2a, b, 5)< R-CHO (6, 7)< View More

Full text of DOI:10.1248/cpb.45.1151

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