Background:
One of the most crucial heterocycles is piperazine for the creation of
novel medication candidates with a variety of medicinal applications. The piperazine moiety is a
cyclic compound with four carbon atoms and two nitrogen atoms in positions 1 and 4.
Objective:
The objective of this studty is the development of 1-((3,4-dimethoxyphenyl) (substitutedphenyl) substituted -piperazine (A1-A10) analogs via the one-pot synthesis method and evaluation for their preliminary antibacterial, antifungal, antimycobacterial, antioxidant, and antimalarial activity.
Methods:
Desired piperazine derivatives were obtained in a single step reaction using piperazine,
aldehydes, and boronic acid derivatives. The structures of all newly synthesized compounds have
been established based on analytical and spectral data. An in silico molecular docking study was
carried out for the series.
Results:
The spectral data using IR, 1
H NMR, and 13C NMR and mass spectra confirmed the
structure of the synthesized compounds. Compounds A6 and A10 were found to be the most promising agents for antimalarial activity. A1-A10 showed a higher IC50 value and found less antioxidant activity. Some of the compounds showed higher potency when compared to the standard
drugs in this antimicrobial study.
Conclusion:
The structure-activity study showed that changes in substituents either on aldehyde,
piperazine, or boronic acid derivatives can lead to potential active compounds. These facts make
the compounds interesting candidates for further evaluation of their efficacy in the treatment of
microbial, tubercular and malarial diseases.