Synthesis, Anti-inflammatory and in silico Studies of few novel 1,2,4-Triazole Derived Schiff Base Compounds

Background:

Every year more than 1 billion prescriptions are written for all NSAIDs and yet the quest to develop new NSAIDs remains prominent.

Objectives:

The current investigation's goal was to synthesize and assess the anti-inflammatory potential of a few more recent 1,2,4-triazole derivatives.

Materials and Methods:

The synthesis of the 1,2,4-triazole compounds (SPG_1-5) was accomplished in three distinct steps involving formation of hydrazide of ibuprofen and followed by cyclization to 1,2,4-triazole nucleus and ultimately formation of Schiff’s base in the final step.

Results:

Each compound was dark brown in color and were obtained in 65-71% yields and was insoluble in water and hexane whereas SPG₂ and SPG₃ were soluble in methanol and all compounds were soluble in chloroform. The compounds were evaluated for in vitro anti-inflammatory potential utilizing albumin denaturation and inhibition of protease action methods. With SPG4 having the best ability to produce the inhibition (62.44±2.889%) at a concentration of 500 g/mL, all the substances showed dosage-dependent inhibition of albumin denaturation. SPG4 was able to inhibit protease activity (46.63±3.211%) at 500 g/mL and the antiprotease efficacy was also dosage-dependent.

Conclusion:

It was evident that the triazole derivatives were able to display moderate anti-inflammatory action and could be optimized to develop lead molecule.