Synthesis, characterization, and biological activity of novel azole piperazine congeners

Priyanka R. Sadalge Vrushabh Karnawadi Lairikyengbam Deepti Roy Manikanda Prabu Geeta Krishnamurthy Pooja Gour Shivanjali Esther Arland Jyotsna Kumar   

Open Access   

Published:  Nov 30, 2022

DOI: 10.7324/JAPS.2023.58094

novel series of piperazine analogs were synthesized comprising azole moieties with good yield. Structures of all four synthesized azole analogs were established by spectral characterization viz 1H-nuclear magnetic resonance, liquid chromatography-mass spectrometry, and FT-IR. Synthesized derivatives were further assessed for their antimicrobial and antioxidant studies. Antimicrobial activity was conducted against Pseudomonas aeruginosa, Staphylococcus aureus, and Candida albicans by well diffusion method. The antimicrobial activity reflects that synthesized piperazine derivatives containing imidazole moiety possess better antibacterial and antifungal activity than piperazine analogs comprising triazole moiety. Staphylococcus aureus exhibited strong resistance over all synthesized piperazine derivatives. Antioxidant activity of synthesized molecules was carried out by using 1, 1-diphenyl-2-picrylhydrazyl. In vitro, antioxidant activity results revealed that IC50 values of synthesized piperazine analogs are comparative with control—gallic acid whereas piperazine derivatives with triazole unit ITZ-1 and ITZ-2 are exhibiting better antioxidant activities. Hence, synthesized novel molecules with better antimicrobial and antioxidant activities may be further used in the formulation of new antimicrobial and antioxidant drugs. Observed IC50, zone of inhibition values, and drug resistance of S. aureus strain against all synthesized novel piperazine derivatives in the present investigation will be helpful to be used as a reference for auxiliary studies and further evaluation is worth developing a new generation drug.

Keyword:     Antimicrobial antifungal imidazole piperazine triazole


Sadalge PR, Karnawadi V, Roy LD, Prabu M, Krishnamurthy G, Gour P, Arland SE, Kumar J. Synthesis, characterization, and biological activity of novel azole piperazine congeners. J Appl Pharm Sci, 2022.

Copyright: © The Author(s). This is an open-access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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