Synthesis, antiaggregant and anticoagulant activity of 2-[3-methyl-8-morpholino-7-(thietanyl-3)xanthinyl-1]acetic acid salts

The purpose of the study was to develop methods for the synthesis of salts of 2-[3-methyl-8-morpholino-7-(thietanyl-3)xanthinyl-1]acetic acid, to study their effect on the hemostatic system, and to predict toxic risks and pharmacokinetic characteristics. 8-Morpholine derivative II was synthesized by reaction of ethyl 2-[8-bromo-3-methyl-7-(thietanyl-3)xanthinyl-1]acetate with morpholine. By hydrolysis of derivative II acid III was obtainedin good yield. Water-soluble salts IVa-g were synthesized using acid III and amines. The structure of synthesized compounds was determined by spectral methods (IR, NMR spectroscopy). According to the computer prediction salts IVa-g should not have toxic risks, most of them satisfy Lipinski's rule of five. In vitro investigation of the antiaggregant and anticoagulant activity of new substances indicated that compounds IVa,d exhibited antiaggregant activity and IVb,f - weak anticoagulant activity.

thietane, morpholine, xanthinyl-1-acetic acid, antiaggregant activity, anticoagulant activity, Lipinski's rule of five