Synthesis of β-lactam nucleoside chimera via Kinugasa reaction and evaluation of their antibacterial activity

Several β-lactam nucleoside chimeras 1 (cis) and 2 (trans) were synthesized from the corresponding N-propargyl nucleobases via Kinugasa reaction in moderate yields. Initial screening for antibacterial activity against ampicillin sensitive E. coli showed weak activity for the uracil-β-lactam chimera.