Synthesis of 2-Furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives as suitable antibacterial agents with mild cytotoxicity

The aim of the present research work was synthesis of some 2-furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives and to ascertain their antibacterial potential. The cytotoxicity of these molecules was also checked to find out their utility as possible therapeutic agents. The synthesis was initiate...

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Veröffentlicht in:Pakistan journal of pharmaceutical sciences 2018-11, Vol.31 (6), p.2477-2485
Hauptverfasser: Abbasi, Muhammad Athar, Nazeer, Muhammad Mubashar, Rehman, Azizur, Siddiqui, Sabahat Zahra, Hussain, Ghulam, Shah, Syed Adnan-Ali, Ahmad, Irshad, Shahid, Muhammad, Sarwar, Muhammad Salman
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container_issue 6
container_start_page 2477
container_title Pakistan journal of pharmaceutical sciences
container_volume 31
creator Abbasi, Muhammad Athar
Nazeer, Muhammad Mubashar
Rehman, Azizur
Siddiqui, Sabahat Zahra
Hussain, Ghulam
Shah, Syed Adnan-Ali
Ahmad, Irshad
Shahid, Muhammad
Sarwar, Muhammad Salman
description The aim of the present research work was synthesis of some 2-furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives and to ascertain their antibacterial potential. The cytotoxicity of these molecules was also checked to find out their utility as possible therapeutic agents. The synthesis was initiated by reacting furyl(-1-piperazinyl)methanone (1) in N,N-dimethylformamide (DMF) and lithium hydride with different aralkyl halides (2a-j) to afford 2-furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives (3a-j). The structural confirmation of all the synthesized compounds was done by IR, EI-MS, H-NMR and C-NMR spectral techniques and through elemental analysis. The results of in vitro antibacterial activity of all the synthesized compounds were screened against Gram-negative (S. typhi, E. coli, P. aeruginosa) and Gram-positive (B. subtilis, S. aureus) bacteria and were found to be decent inhibitors. Amongst the synthesized molecules, 3e showed lowest minimum inhibitory concentration MIC = 7.52±0.μg/mL against S. Typhi, credibly due to the presence of 2-bromobenzyl group, relative to the reference standard, ciprofloxacin, having MIC = 7.45±0.58μg/mL.
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title Synthesis of 2-Furyl[(4-aralkyl)-1-piperazinyl]methanone derivatives as suitable antibacterial agents with mild cytotoxicity
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