AI Article Synopsis
- Eleven azide oximes were synthesized and tested for their ability to inhibit blood platelet aggregation, with nine of them showing significant effects, especially azido-4-nitrophenylbenzaldoxime (2h) which had the strongest potency at an IC50 of 2 microM.
- Nine of the compounds demonstrated notable antithrombotic properties, particularly compounds 2h and 2c, which inhibited thrombus formation by over 20% after a single dose and also lowered blood pressure in hypertensive rats.
- Seven of the azide oximes were converted to tetrazoles, but these showed less effectiveness in preventing thrombosis; additionally, the azide oximes were found to release nitric oxide and nitrosohyd
Article Abstract
Eleven azide oximes were prepared and tested for their antiplatelet (in vitro), antithrombotic, and blood pressure lowering activities. Nine of them inhibited the aggregation of blood platelets (Born test, inducer collagen) with IC50 values between 10 and 50 microM. The most active compounds i.e. azido-4-nitrophenylbenzaldoxime (2h) had an IC50 = 2 microM. Nine azide oximes exhibited significant antithrombotic properties. The most active compounds were 2h and 2c (azido-4-methylphenylbenzaldoxime) with an inhibition of thrombus formation above 20% in arterioles after a single p.o. dose of 60 mg/kg. Both compounds lowered the blood pressure in spontaneously hypertensive rats by 11% (2h) or 5% (2c), respectively. Seven azide oximes were rearranged to the title tetrazololes which however showed smaller antithrombotic effects. In separate in vitro experiments at 37 degrees C it could be demonstrated that azide oximes release nitric oxide (conversion rate approximately 10%.h-1) and nitrosohydrogen (conversion rate approximately 2%.h-1). This makes it appear probable that the above effects are mediated by these molecules.
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| http://dx.doi.org/10.1002/1521-4184(20006)333:6<157::aid-ardp157>3.0.co;2-c | DOI Listing |
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