EX VIVO ANTICOAGULANT ACTIVITY OF 1, 3, 4-OXADIAZOLE DERIVATIVES

摘要

Objective: The present medication for the management of arterial thromboembolism (ATE) disorders by anticoagulant therapy highlights its lacunae due to recurrent ATE episodes and indicates the need for better anticoagulant agents with clinical advantage. Methods: The anticoagulant study was performed for increase in prothrombin time (PT) and activated partial thromboplastin time (aPTT) at a test dose of 25 mg kg -1 . Results: The results of ex vivo anticoagulant evaluation revealed that the tested compounds 3a-3q did not exhibit a significant increase in PT with respect to acenocoumarol (1 mg kg -1 ) employed as the reference drug for increase in PT. While the compounds, 3a-3q exhibited minimal increase in aPTT in comparison to unfractionated heparin (500 IU kg -1 ) employed as the reference drug for increase in aPTT. Among all the tested compounds, only compound 3q exhibited moderate anticoagulant activity with an increase in PT (33 ± 0.4 s) to that of the reference drug acenocoumarol (48 ± 0.5 s). Conclusion: The anticoagulant efficacy investigation highlights that the synthesized compound 3q could be considered for further clinical studies to ascertain its possible hit as anticoagulant agents. Keywords: 1,3,4-Oxadiazole, Activated Partial Thromboplastin Time, Benzofuran, Prothrombin Time.