Affiliation:
1. Department of Chemistry, M.S. Ramaiah University of Applied Sciences, Karnataka, 560058, Bangalore, India
Abstract
Introduction:
In this study, a series of novel piperazine derivatives were synthesised with high-to-good
yields, and their structural analogies were confirmed using FTIR, 1H-NMR, and LC-MS techniques.
Methods:
The synthesised compounds were evaluated for antioxidant and antimicrobial activities. Among the four
synthesised piperazine derivatives, compound PD-2 exhibited relatively good antioxidant activity, with an IC50
value of 2.396 μg/mL, while the other three derivatives showed moderate to low antioxidant activity. Furthermore,
compound PD-2 displayed antimicrobial activity against Pseudomonas aeruginosa, a gram-negative bacterium,
and Candida albicans, a fungus. However, all four compounds showed strong resistance against grampositive
bacteria, Staphylococcus aureus.
Results:
Additionally, compound PD-1 exhibited significant antihistamine activity, eliciting an 18.22% reduction
in histamine levels. Both PD-1 and PD-2 demonstrated noteworthy anti-inflammatory activity in a dosedependent
manner (5-10 μM), leading to the inhibition of nitrite production up to 39.42% and 33.7% at higher
concentrations (10 μM) and inhibition of tumour necrosis factor-alpha (TNF-α) generation up to 56.97% and
44.73% at 10 μM, respectively. Additionally, both novel molecules PD-1 and PD-2 effectively restrained the
growth of HepG2 cells in a manner that is dependent on the dosage up to 55.44% and 90.45% at the highest concentrations
(100 μg/mL), respectively.
Conclusion:
These findings substantiate the rationale for further investigation into the novel series of persuasive
piperazine analogues as potential agents with anti-inflammatory, antihistamine and anticancer properties.
Publisher
Bentham Science Publishers Ltd.