Abstract
A series of novel piperazine-1,2,3-triazole derivatives, which entailed the bioisosteric replacement of the imidazole moiety and hybridization of two drug scaffolds was prepared by employing the regioselective copper (I)-catalysed azide-alkyne 1,3-dipolar cycloaddition reaction. The synthesized compounds were evaluated for antibacterial activities against Gram-negative (E. Coli and P. Putida), Gram-positive S. Aureus bacteria and fungicidal activities against F. oxysporum, F. gramillarium and F. monalliforme fungi. Compound 7ac′ exhibited moderate but promising antibacterial activity against Gram-negative bacteria and fungicidal activity against F. oxysporum and F. gramillarium.
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The authors thank UGC, New Delhi [Grant No. 39-733/2010 (SR)], for financial support. PK and KP thank UGC, New Delhi, for junior research fellowships.
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Khedar, P., Pericherla, K., Singh, R.P. et al. Click chemistry inspired synthesis of piperazine-triazole derivatives and evaluation of their antimicrobial activities. Med Chem Res 24, 3117–3126 (2015). https://doi.org/10.1007/s00044-015-1361-5
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DOI: https://doi.org/10.1007/s00044-015-1361-5