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

• Published in: Pakistan Journal of Pharmaceutical Sciences
• Main Author: Abbasi M.A.; Nazeer M.M.; Aziz-Ur-Rehman; Siddiqui S.Z.; Hussain G.; Shah S.A.A.; Ahmad I.; Shahid M.; Sarwar M.S.
• Format: Article
• Language: English
• Published: Pakistan Journal of Pharmaceutical Sciences 2018
• Online Access: https://www.scopus.com/inward/record.uri?eid=2-s2.0-85055182626&partnerID=40&md5=259dd2e1a8bd5279441a69ff821112fe

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, 1H-NMR and 13C-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. © 2018 Pakistan Journal of Pharmaceutical Sciences. All rights reserved.