New NO-donors with antithrombotic and vasodilating activities .13. Pyrazol-4-one 1,2-dioxides and 4-hydroxyiminopyrazole 1,2-dioxides

Twenty pyrazol-4-one 1,2-dioxides and eleven 4-hydroxyimino-pyrazole 1,2-dioxides were prepared and tested for their anti-platelet activity (Born test with collagen). Six compounds which al belong to the pyrazolone series inhibited the platelet aggregation half-maximally in submicromolar concentrati...

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Published inArchiv der Pharmazie (Weinheim) Vol. 328; no. 11-12; pp. 765 - 769
Main Authors Rehse, K, Muller, U
Format Journal Article
LanguageEnglish
Published DEERFIELD BEACH Wiley 01.12.1995
Subjects
Chemistry
Chemistry, Medicinal
Chemistry, Multidisciplinary
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
pyrazolones
1,2-dioxides
ACCOUNTS
antithrombotic properties
inhibition
OLIGOAMINES
platelet aggregation
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Summary:Twenty pyrazol-4-one 1,2-dioxides and eleven 4-hydroxyimino-pyrazole 1,2-dioxides were prepared and tested for their anti-platelet activity (Born test with collagen). Six compounds which al belong to the pyrazolone series inhibited the platelet aggregation half-maximally in submicromolar concentrations (200-800 nmol/L). In positions 3 and 5, these compounds bear at least one (15, 16, 24, 31) or two substituents (7, 29) with electron-withdrawing groups. Among them are aromatic moieties like 4-hydroxysulfonylphenyl (7), 4-cyanophenyl (16), 4-chlorophenyl (15), phenyl (24) or carboxylic acid esters (29). Two compounds were investigated in an in vivo thrombosis model (1, 31). 2h after oral administration of 60 mg/kg 1 to rats in arterioles 69% inhibition of thrombus formation (venules 40%) was observed.
ISSN:0365-6233
DOI:10.1002/ardp.19953281107