Sparsomycin Analogs. III. Synthesis and Biological Activities of (E)-β-(6-Methyluracil-5-yl) acrylic Acid Derivatives

抄録

In order to study the structure-activity relationship of sparsomycin, an antitumor antibiotic, 26 sparsomycin analogs (3-5) were synthesized and their antibacterial activities and lytic actions on Ehrlich ascites carcinoma cells were tested. It was found that N-[(E)-β-(6-methyluracil-5-yl) acryloyl]-S-methyl-D-cysteinol (5g) and N-[(E)-β-(6-methyluracil-5-yl) acryloyl]-D-methioninol (5i) showed significant antibacterial activity (minimum inhibitory concentration 25 μg/ml) against Streptococcus pyogenes.