DERIVATIVES OF 2,3,4,5-TETRAHYDRO[1,3]DIAZEPINO[1,2-A]BENZIMIDAZOLE, POSSESSING ANTIAGREGANT ACTIVITY

Issue: 
8
Year: 
2015

A.F. Kucheryavenko
Dr.Sc. (Med.), Associate Professor, Сhair of Pharmacology, Volgograd State Medical University
O.A. Salaznikova
Ph.D. (Med.), Senior Lecturer, Сhair of Pharmacology, Volgograd State Medical University
V.S. Sirotenko
Intern, Volgograd State Medical University
K.A. Gajjdukоva
Student, Volgograd State Medical University
A.A. Spasov
Dr.Sc. (Med.), Professor, Academician of RAS, Honored Master of Sciences,
Head of the Сhair of Pharmacology, Volgograd State Medical University
L.N. Divaeva
Ph.D. (Chem.), Senior Research Scientist, Institute of Physical and Organic Chemistry, South Federal University (Rostov-on-Don)
T.A. Kuz’menko
Ph.D. (Chem.), Senior Research Scientist, Institute of Physical and Organic Chemistry, South Federal University (Rostov-on-Don)
V.A.Anisimova
Ph.D. (Chem.), Leading Research Scientist, Institute of Physical and Organic Chemistry, South Federal University (Rostov-on-Don)

Platelet activation is an integral component of the pathophysiolody that leads to thrombotic and ischemic diseases such as myocardial infarction, cerebral stroke, and peripheral vascular disease. To develop more safe and effective antiplatelet agents may be promising approach for prevention and treatment of atherothrombosis Determination of antiplatelet activity of the novel of 2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole derivatives in vitro and in vivo. Antiaggregatory activity of the novel of 2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole derivatives in vitro and in vivo has been investigated in comparison to antiaggregant drug acetylsalicylic acid (ASA) using the turbidimetry method of ADP- induced aggregation of platelets in male rabbits and rats [ Gabbasov, 1989]. Etalon antiaggregant drug acetylsalicylic acid and the investigated compounds revealed dose-dependent antiaggregatory activity in vitro 2 the novel diazepino[1,2-a]benzimidazole derivatives excelled acetylsalicylic acid in action. IC50 DAB-25, DAB-7 and acetylsalicylic acid − 1,9∙10−5 М, 7,3∙10−5 M and 1,04∙10‒4 M respectively. Stadies have shown that DAB-25 has inhibitory effect on rat platelet aggregation by 2,8 times compare with acetylsalicylicum acide. These findings demonstrate that new derivative of 2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole are perspective class of antirhtombogenic drugs.

Keywords: 
Keywords: antiaggregatory action
platelet aggregation
acetylsalicylic acid.