SYNTHESIS AND IMPACT OF THE SALTS OF 2-[3-METHYL-7-(1- OXOTHIETANYL-3)-1-ETHYLXANTHINYL-8-THIO]ACETIC ACID ON HEMOSTASIS SYSTEM

Abstract

2-[3-methyl-7-(1-oxothietanyl-3)-1-ethylxanthinyl-8-thio]acetic acid was synthesized with 76% yields by reaction of 8-bromo- 3-methyl-7-(1-oxothietanyl-3)-1-ethylxanthine with the thioglycolic acid. The salts of 2-[3-methyl-7-(1-oxothietanyl-3) )-1- ethylxanthinyl-8-thio]acetic acid were obtained with 70 - 95% yield by interaction of the synthesized acid with the different bases. The structure of the synthesized compounds was confirmed by IR, NMR spectroscopy. We have carried out a screening of impact of firstly sythesized derivatives and medically applied therapeutic agents on the hemostasis system under conditions in vitro with donated human blood. ADP- and collagen-induced platelet aggregations were registered. We evaluated the general nature of the aggregation, the maximum aggregate, maximum aggregation rate, the average size of platelet aggregates. The study of new compounds and comparative medicines was made with concentration of 2×10-3 mol/L. It shows differences in impact of the compounds on hemostatic system. It was established that most synthesized compounds exhibit potentially high antiaggregation activity. At collagen-induced aggregation, all studied compounds showed antiaggregation activity, but neither aspirin nor pentoxifylline showed activity in these conditions. The findings prove that it is neccessary and up-to-date to continue research of this set of derivatives influencing the hemostasis system as potential antiplatelets and haemostatic agents.