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Article
Antiplatelet and Antithrombotic Properties of Compound L-36, a 6H-1,3,4-Thiadiazine Derivative
Compound L-36, a new derivative of 6H-1,3,4-thiadiazine, was studied in in vitro and in vivo experiments. This compound exhibits high antiplatelet and antithrombogenic activity. In in vitro experiments, compound ...
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Article
Bioavailability of the Tablet Dosage Form of a Benzimidazole Derivative Possessing Antiplatelet Activity
The bioavailability of the tablet dosage form of pharmaceutical substance RU-891, i.e., 9-(3,4-dihydroxyphenacyl)-2,3-dihydroimidazo[1,2-a]benzimidazole hydrobromide, was investigated. The main pharmacokinetic pa...
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Article
Antiplatelet Activity of Riamilovir under Conditions of Lipopolysaccharide Intoxication
We studied the effect of antiviral agent riamilovir on ADP-induced platelet aggregation in the absence and presence of LPS. Unlike acetylsalicylic acid (reference drug), riamilovir did not exhibit antiplatelet...
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Article
Pharmacological Properties of 2-Aminobenzimidazole Halides and Imidazo[1,2-a]Benzimidazole Derivatives
Halides of 2-aminobenzimidazolium and derivatives of 9-substituted 2-(4-fluorophenyl)imidazo[1,2-a]benzimidazoles have been studied for ten types of biological activity in vitro. Among the aminobenzimidazolium de...
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Article
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 comorbiditie...
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Article
Quantitative Determination of Angipur Drug Substance in Blood Plasma by HPLC with Fluorescence Detection
A quantitative determination method using HPLC with fluorescence detection for the xanthine derivative 3-methyl-8-(piperazin-1-yl)-7-(thietan-3-yl)-1-ethyl-1H-purine-2,6(3H,7H)-dione hydrochloride (Angipur drug s...
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Article
Biopharmaceutical Study of an Injectable Dosage Form of the New Antiaggregant Substance 3-Methyl-8-(Piperazin-1-yl)-7-(Thietan-3-yl)-1-Ethyl-1H-Purine-2,6(3H,7H)-Dione Hydrochloride
The pharmacokinetic parameters of the parent substance and the injectable dosage form of the new antiplatelet drug 3-methyl-8-(piperazin-1-yl)-7-(thietan-3-yl)-1-ethyl-1H-purine-2,6(3H,7H)-dione hydrochloride in ...
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Article
In silico consensus activity prediction, rational synthesis, and evaluation of antiglycation and antiplatelet activities of 3,6-disubstituted 1,2,4,5-tetrazines
According to the in silico consensus activity prediction, a series of 3,6-disubstituted 1,2,4,5-tetrazines were synthesized as promising inhibitors of the Maillard reaction. In addition to the studies of antiglyc...
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Article
Uracil Hydroxybenzamides as Potential Antidiabetic Prodrugs
A series of N1, N3-bis-hydroxybenzoyl, -acetoxybenzoyl, and -methoxybenzoyl uracil derivatives were synthesized. All compounds were screened for the ability to rupture protein cross links and antiglycating, chela...
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Article
Antithrombotic Activity of a Novel Diazepino[1,2-α] Benzimidazole Derivative on Arterial Thrombosis Model in Rats without Concomitant Pathology and in Rats with Experimental Myocardial Infarction
Antithrombotic activity of a novel tricyclic derivative of diazepino[1,2-α]benzimidazole (DAB-15) was examined on the model of arterial thrombosis developed in rats without concomitant pathology and in rats wi...
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Article
Evaluation of N-Hydroxy-, N-Metoxy-, and N-Acetoxybenzoyl-Substituted Derivatives of Thymine and Uracil as New Substances for Prevention and Treatment of Long-Term Complications of Diabetes Mellitus
New uracil and thymine derivatives, N1-,N3- and N1,N3-(RO-benzoyl)-(1H,3H)-pyrimidine- 2,4-diones, were synthesized (RO- is hydroxy, acetoxy- or methoxy-group). The compounds were studied in a complex of in vitro...
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Article
Synthesis and Pharmacological Activity of Trifluoromethyl-Containing Imidazo[1,2-A]Benzimidazoles
A series of 2-(4-trifluoromethylphenyl)- and 2-trifluoromethyl-9-dialkylaminoalkylimidazo[1,2-a]benzimidazoles were synthesized for the first time by reacting 2-amino-1-dialkylaminoalkylbenzimidazoles and 2-bromo...
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Article
The Search for Pharmacologically Active Compounds Among the 2-Dialkylaminobenzimidazoles
Heating of substituted benzimidazole-2-sulfonic acids in the presence of excess quantities of secondary amines was used to synthesize dialkylaminobenzimidazoles. Experimental studies of potential antiarrhythmi...
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Article
Effect of Compound Sbt-828, a New Indole Derivative Exhibiting Antiaggregant Activity, on the Prostacyclin—Thromboxane A2 Balance
We investigated the effect of a new indole derivative Sbt-828 with antiaggregant properties on prostacyclin-generating activity of the vascular wall and thromboxane A2 level in platelets of intact rats. The subst...
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Article
Antithrombotic Activity of DAB-15, a Novel Diazepinobenzimidazole Compound
Antithrombotic activity of a new orally administered antiplatelet compound DAB-15 was compared to that of acetylsalicylic acid, ticlopidine, and clopidogrel in the experimental model of arterial thrombosis in ...
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Article
Effect of a New Antioxidant Enoxifol on Platelet Aggregation and Blood Rheological Properties in Rats with Experimental Diabetes Mellitus
Effect of a new antioxidant enoxifol exhibiting antiplatelet activity in vitro and in vivo on hemostasis parameters was assessed in laboratory rats with experimental diabetes mellitus. Gliclazide, a hypoglycemic ...
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Article
1-Substituted 2-Benzylaminobenzimidazoles with Phenyl Methoxyls: Synthesis, Computer Prediction, and Pharmacological Activity
Condensation of 1-substituted 2-aminobenzimidazoles with aromatic aldehydes produced the corresponding azomethines, reduction of which by sodium borohydride afforded 1-substituted 2-benzylaminobenzimidazoles. ...
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Article
Prototropic equilibrium in 1(11)H-2, 3, 4, 5-tetrahydro[1, 3]diazepino[1, 2-a]benzimidazole, synthesis and pharmacological properties of its N-substituted derivatives
Based on the X-ray crystallography and 1H NMR spectroscopy data and quantum chemical studies, it was found that 1(11)H-2, 3, 4, 5-tetrahydro[1, 3]diazepino[1, 2-a]benzimidazole (1) exists almost exclusively in th...
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Article
Antithrombotic Activity of a New Hypoglycemic Compound Limiglidole in Mouse Model of Cell Thrombosis
Antithrombotic activity of hypoglycemic compound limiglidole that exhibits antiplatelet activity 2-fold exceeded activity of antiplatelet agent acetylsalicylic acid in the mouse model of systemic collagen–epin...
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Article
Antithrombotic Activity of a New Benzimidazole Derivative in the Thrombosis Model in Mice
Antithrombotic activity of a new benzimidazole derivative RU-891, characterized by antiaggregant activity, vs. reference drug acetylsalicylic acid was studied on the epinephrinecollagen thrombosis model in mice. ...