Synthesis of 4,5-functionalized-2-methyl-6-(substituted aryl)-3(2H)-pyridazinones: A new group of potent platelet aggregation inhibitors

A series of 4,5-functionalized-2-methyl-6-(substituted phenyl)-3(2H)-pyridazinones were synthesized and evaluated as platelet aggregation inhibitors in human platelet rich plasma (PRP). The new products generally displayed significant higher activity with respect to the corresponding unsubstituted a...

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Bibliographic Details
Published inFarmaco (Società chimica italiana : 1989) Vol. 52; no. 3; pp. 173 - 178
Main Authors DalPiaz, Ciciani, G, Giovannoni, MP
Format Journal Article
LanguageEnglish
Published ROME Soc Chimica Italiana 01.03.1997
Subjects
Animals
Blood Platelets - drug effects
Blood Platelets - metabolism
Cyclic AMP - metabolism
Humans
In Vitro Techniques
Life Sciences & Biomedicine
Male
Molecular Structure
Pharmacology & Pharmacy
Platelet Aggregation Inhibitors - chemistry
Platelet Aggregation Inhibitors - pharmacology
Pyridazines - chemistry
Pyridazines - pharmacology
Rats
Science & Technology
Structure-Activity Relationship
PHOSPHODIESTERASE-III
AGENTS
MODEL
BIPYRIDINE
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Summary:A series of 4,5-functionalized-2-methyl-6-(substituted phenyl)-3(2H)-pyridazinones were synthesized and evaluated as platelet aggregation inhibitors in human platelet rich plasma (PRP). The new products generally displayed significant higher activity with respect to the corresponding unsubstituted aryl compounds. Compounds 27 and 31 appeared of particular interest, being their IC50s, in the submicromolar range. Structure-activity relationships (SARs) are discussed.
ISSN:0014-827X
1879-0569