EX VIVO ANTICOAGULANT ACTIVITY OF 1, 3, 4-OXADIAZOLE DERIVATIVES
Keywords:
1, 3, 4-Oxadiazole, Activated Partial Thromboplastin Time, Benzofuran, Prothrombin TimeAbstract
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.
Â
Downloads
References
Murray CJ, Lopez AD. Global mortality, disability, and the contribution of risk factors: global burden of disease study. Lancet 1997;349:1436–42.
Groth T, Wagenknecht W. Anticoagulant potential of regioselective derivatized cellulose. Biomater 2001;22:2719-29.
Hirsh J, Dalen JE, Anderson DR, Poller L, Bussey H, Ansell J, et al. Oral anticoagulants: mechanism of action, Clinical Effectiveness, and Optimal Therapeutic Range. Chest 2001;119:8-21.
Cain D, Hutson SM, Wallin RJ. Assembly of the warfarin-sensitive vitamin k 2,3-epoxide reductase enzyme complex in the endoplasmic reticulum membrane. Biol Chem 1997;272:29068-75.
Vishwanathan B, Gurupadayya BM, Sairam KV, Inturi BK. Design, synthesis, in vitro antioxidant and in vivo anti-inflammatory activities of novel oxadiazole derivatives. Int J Pharm Pharm Sci 2014;6:514-20.
Sztaricskai F, Takacs IE, Pusztai F, Szabo G, Csipo I. Antiulcer effect of the N-and O-β-D-glucopyranosides of 5-aminosalicylic acid. Arch Pharm 1999;332:321–6.
Shi S, Wang Z, Guo S, Li L. Anticoagulant activity of cellulose sulfates with different intrinsic viscosities. Asian J Pharm Sci 2007;2:38-43.
Couri D, Wosilait WD. The effect of coumarin anticoagulants on the adenine nucleotide content and protein synthesis in rat liver. Biochem Pharmacol 1966;15:1349-60.