1957 年 77 巻 1 号 p. 94-98
Relationship between chemical structure and antibacterial activity was examined with the dehydroacetic acid-type and 3-acyl-4-hydroxycoumarin-type compounds, which are pyrone derivatives. It is known that the introduction of an acyl group in the 3-position of triacetic acid lactone and 4-hydroxycoumarin results in marked increase of antibacterial action. In the present series of experiments, the effect of change in acyl side chain into 3-position of pyrone derivatives, which possess all the requisite conditions thought to be necessary for the appearance of antibacterial activity, on antibacterial activity was examined. The compounds synthesized and submitted for antibacterial tests were 12 kinds of substances possessing ethoxycarbonyl group or carboxyl group at the terminal end of the acyl group in 3-position of triacetic acid lactone and 4-hydroxycoumarin. It was thereby found that these pyrone derivatives possessed lower antibacterial activity than that of corresponding acyl compounds and the degree of such lowering was the more marked in the carboxyl series.