Synthesis and antimicrobial activity of N-alkyl and N-aryl piperazine derivatives

N-Alkyl and N-aryl derivatives of piperazines have been synthesized and screened for antibacterial and antifungal activities. All the synthesized compounds show potent antibacterial activity and were found to be less active against fungi. Compounds 4d and 6a were found to be very less toxic to human...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2006-03, Vol.14 (6), p.1819-1826
Main Authors: Chaudhary, Preeti, Kumar, Rupesh, Verma, Akhilesh K., Singh, Devender, Yadav, Vibha, Chhillar, Anil K., Sharma, G.L., Chandra, Ramesh
Format: Article
Language:English
Subjects:
Anti-Infective Agents - chemical synthesis
Anti-Infective Agents - chemistry
Anti-Infective Agents - pharmacology
Antibacterial
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antifungal
Antifungal agents
Aspergillus flavus
Aspergillus fumigatus
Aspergillus niger
Bacteria - drug effects
Biological and medical sciences
Cytotoxicity
Erythrocytes - drug effects
Escherichia coli
Fungi - drug effects
General aspects
Humans
Medical sciences
Microbial Sensitivity Tests
Molecular Structure
Pharmacology. Drug treatments
Piperazine
Piperazines - chemical synthesis
Piperazines - chemistry
Piperazines - pharmacology
Pseudomonas aeruginosa
Staphylococcus aureus
Streptomyces
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Summary:N-Alkyl and N-aryl derivatives of piperazines have been synthesized and screened for antibacterial and antifungal activities. All the synthesized compounds show potent antibacterial activity and were found to be less active against fungi. Compounds 4d and 6a were found to be very less toxic to human erythrocytes when compared with gentamicin. A series of substituted piperazine derivatives have been synthesized and tested for antimicrobial activity. The antibacterial activity was tested against Staphylococcus aureus (MTCCB 737), Pseudomonas aeruginosa (MTCCB 741), Streptomyces epidermidis (MTCCB 1824) and Escherichia coli (MTCCB 1652), and antifungal activity against Aspergillus fumigatus, Aspergillus flavus and Aspergillus niger. All synthesized compounds showed significant activity against bacterial strains but were found to be less active against tested fungi. In vitro toxicity tests demonstrated that compounds 4d and 6a showed very less toxicity against human erythrocytes.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2005.10.032