One pot Facile Synthesis of Anti-microbial β-Lactam Derivatives Catalysed by Fe(acac)3

We have developed novel route for the synthesis of β-Lactam by Fe(acac)3 based catalytic system with > 90% yield. It is one pot Knoevenagel condensation of aldehyde with ethyl cyanoacetate followed by chemoselective reduction of the nitrile substituted C=C bond and nitrile functional group with sodium borohydride.Anti-microbial activity of the compounds exhibited at lower concentration against gram positive, gram negative bacteria and yeast with minimum inhibitory coIncentration (MIC) as low as 16 µg/mL. Compound have low hemolytic activity at their respective MIC. These derivatives might be liable to be increase the permeability of the bacterial cell membrane, which was demonstrated by DAPI, FITC, PI uptake studies and atomic force microscopy imaging of the treated cells. One pot synthesis with anti-microbial activity of β-Lactam derivatives can be helpful to developed effective antibacterial agents.

Keywords:

Fe(acac)3 , Knoevenagel condensation , β-Lactam , anti-microbial , FITC , AFM