Sparsomycin analogs. III. Synthesis and biological activities of (E)-.BETA.-(6-methyluracil-5-yl)acrylic acid derivatives.

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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.

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