Antithrombotic Activity of the Antiplatelet Agent Angipur on the Model of Arterial Thrombosis in Rats with Isoproterenol-Induced Myocardial Infarction.

We studied the effect of Angipur on the process of experimental thrombosis induced by damage to the carotid artery wall by surface application of 50% ferric chloride (III) solution in rats without comorbidities and with isoproterenol-induced myocardial infarction. In animals without comorbidities, Angipur administered intravenously was 1.2 times less effective, in terms of ED50, than the well-known inhibitor of GPIIb/IIIa platelet receptors tirofiban. However, under conditions of non-coronary myocardial infarction, Angipur significantly prolonged the time of thrombus formation and exhibited 1.4-fold higher activity than the reference drug tirofiban.

Synthesis and Antiplatelet and Anticoagulant Activity of Thietane-Containing 2-(5-Bromo-2,4-Dihydro-3-Oxo-1,2,4-Triazolyl-4)Acetate Salts.

Sulfone II was synthesized via oxidation of ethyl 2-[5-bromo-2,4-dihydro-3-oxo-2-(thietanyl-3)-1,2,4-triazolyl- 4]acetate (I) by H2O2. Hydrolysis of esters I and II synthesized 2-[5-bromo-2,4-dihydro- 3-oxo-2-(thietanyl-3)-1,2,4-triazolyl-4]- and 2-[5-bromo-2,4-dihydro-3-oxo-2-(1,1-dioxothietanyl-3)-1,2,4- triazolyl-4]acetic acids III and IV, respectively.Water-soluble salts V and VI were prepared by reacting acids III and IV with alkali-metal hydroxides and amines. The structures of the synthesized compounds were confirmed IR and NMR spectroscopic data. The antiplatelet and anticoagulant activity of the synthesized compounds was studied in vitro based on predictions of the PASS computer program. Compounds III and VIb, which showed the absence of predicted toxic risks and were superior to the reference drug in the collagen-induced aggregation test, had the most pronounced antiplatelet activity (comparable to that of acetylsalicylic acid) in the ADP-induced aggregation test. The anticoagulant activity of the compounds was significantly inferior to that of heparin sodium. All synthesized compounds satisfied Lipinski's rule-of-5.

Changes in electrokinetic properties of erythrocytes under the influence of pentoxifylline and new hemorheologically active substances.

We studied the impact of compounds RU-1202 and SUM-55 on electrophoretic mobility of "young" and "old" erythrocytes fractionated in a density gradient. The test compounds are shown to increase electrophoretic mobility of erythrocytes, compound SUM-55 being superior to the reference drug pentoxifylline.

[Hemorheological properties of new xanthine derivative studied on model of streptozotocin induced diabetes mellitus].

Influence of a new xanthine derivative SUM-55 on microrheological properties erythrocytes in rats with experimental diabetes has been investigated. It is shown that compound SUM-55 significantly reduces aggregation and increases deformability of erythrocytes. Comparative analysis showed that SUM-55 is comparable with pentoxyphylline in the ability to reduce aggregation of erythrocytes and is superior to the reference drug in increasing deformability of red bloodcells.

[6,8-Dimethyl-2-piperidinomethyl-2,3-dihydrothiazolo[2,3-f]xanthine: a new inductor of the monooxygenase system inhibits experimental intrahepatic cholestasis in rats]. / Novyi induktor monooksigenaznoi sistemy 6,8-dimetil-2-piperdinometil-2,3-digidrotiazolo[2,3-f]ksantin kak korrektor vnutripechenochnogo kholestaza v ékperimente.

6,8-Dimethyl-2-piperidinomethyl-2,3-dihydrothiazolo[2,3-f]xanthine, a new inductor of the monooxygenase system, inhibited the development of experimental intrahepatic cholestasis induced by alpha-naphthylisothiocyanate in rats. The drug stimulated the detoxicating function of liver, increased the survivability of rats, restored the level of microsomal protein and cytochrome P-450, decreased the cell-average erythrocyte fragility, and reduced the activity of cholestasis markers and the amount of TBA-active products in hepatocytes.