Article

Thrombolytic activity of 1,3,4-oxadizole derivatives

Author : B. Vishwanathan and B.M. Gurupadayya

The currently available medication for management of arterial thromboembolism (ATE) disorders by antithrombotic therapy highlights its lacunae due to recurrent ATE episodes and indicates the need for better thrombolytic agents with clinical advantage. In the present study, a series of 1,3,4-oxadiazole derivatives (3a-3q) derived from benzofuran were evaluated for in vitro clot lysis study for thrombolytic activity. The thrombolytic evaluation was performed for decrease in solid clot weight by the clot lysis process at a concentration of 6.25, 12.5 and 25 M strength. The results of in vitro clot lysis for thrombolytic evaluation revealed that the tested compounds 3a-3q exhibited significant clot lysis with respect to streptokinase (30,000 IU) employed as reference drug. Among all the tested compounds, compound 3o, 3n and 3m exhibited potent thrombolytic activity with ED50 value of 18.8, 20.4 and 20.9 M, respectively. The thrombolytic efficacy investigation highlights that the synthesized compound 3o could be considered for further clinical studies to ascertain its possible hit as thrombolytic agents.


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