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In search of new biologically potent molecules a small focused library of new guanidine-1,2,3-triazole hybrid derivatives were synthesized  via  Organocatalytic enolate- mediated azide-carbonyl [3 + 2] cycloaddition yielding a highly functionalized triazole core structure. The synthesis of all the derivatives were confirmed by spectral analysis  1 H NMR,  13 C NMR and MS. The new guanidine-1,2,3-triazole conjugates were found to exhibit promising anti-inflammatory and antioxidant activity. The anti-inflammatory activity screened by membrane stabilization method summarizes the four potential conjugates  5c ,  5f ,  5h  and  5g  to be potent in comparison with standard drug Diclofenac sodium ( DFS ). The conjugates were also assessed for antioxidant potential by DPPH method. Among all the synthesized compounds, the compounds  5d ,  5f ,  5g  and  5h  exhibited potent antioxidant activity. Molecular docking study was performed to gain insight into the putative binding mode and binding strength of these compounds with the target enzyme Cyclo-oxygenase (COX-2) enzyme. The  in vitro  and  in silico  studies together with simpler designing and synthesis strategy  via  Organocatalytic enolate- mediated azide-carbonyl [3 + 2] cycloaddition followed by a two-component reaction with guanidine in basic conditions rationalize guanidine-1,2,3-triazole hybrid derivatives as easily assessable novel therapeutic agents.

Design, Synthesis and Bioevaluation of Highly Functionalized 1,2,3-Triazole-Guanidine Conjugates as Anti-Inflammatory and Antioxidant Agents