New NO-donors with antithrombotic and vasodilating activities, IX: Thiadiazole nitrosimines.
Twenty 1,3,4-thiadiazole-2-nitrosimines and two 1,2,4-thiadiazole-5-nitrosimines were synthesized and assayed in the Born-test for their antiplatelet activity. Only two 1,3,4-thiadiazoles inhibited the aggregation at IC50 < 10 mumol/L. In an in vivo thrombosis model only in arterioles a small inhibition of thrombus formation was observed. The poor test results correspond to a very high chemical stability of the titel nitrosimines.
Rehse
K
K
Institut für Pharmazie, Freien Universität Berlin.
Lüdtke
E
E
D000818:Animals; D005343:Fibrinolytic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D009602:Nitrosamines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D014665:Vasodilator Agents / Q000138:chemical synthesis* / Q000494:pharmacology
D005343:Fibrinolytic Agents; D009602:Nitrosamines; D013830:Thiadiazoles; D014665:Vasodilator Agents