2-Nitrobenzofuran誘導体の化学療法学的研究

概要

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Antibacterial activities of 2-nitrobenzofuran derivatives (NBFD) against 8 strains of gram-possitive and -negative bacteria were comparable to nitrofurantoin, or somewhat more potent than that. Elongated cells were occasionally observed in the culture medium containing NBFD. When NBFD (12.5-100 mg/kg) was orally administered to rats, the metabolites excreated in urine also showed antibacterial activity. The antibacterial spectrum of the urinary metabolites, however, was different from that of the intact compound. The cytotoxicity of NBFD and nitrofurantoin was examined using cultured chick embryo fibroblasts. The inhibition of cell multiplication appeared in the concentration range of 0.39-25μg/ml. It was noted that in the case of 7-substituted NBFD the compound which possesed a high antibacterial activity indicated a low cytotoxicity. A reverse relationship between antibacterial activity and cytotoxicity seemed to depend on the size of a substituent in the 7-position of NBFD.
公益社団法人日本薬学会の論文
1978-03-25