Synthesis of beta-lactam nucleoside chimera via Kinugasa reaction and evaluation of their antibacterial activity.
Several beta-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-beta-lactam chimera.
Basak
Amit
A
Department of Chemistry, Indian Institute of Technology, Kharagpur 721302, India. absk@chem.iitkgp.ernet.in <absk@chem.iitkgp.ernet.in>
Pal
Runa
R
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004926:Escherichia coli / Q000187:drug effects / Q000254:growth & development; D009705:Nucleosides / Q000138:chemical synthesis* / Q000494:pharmacology; D047090:beta-Lactams / Q000138:chemical synthesis* / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D009705:Nucleosides; D047090:beta-Lactams