1‐Hydroxypiperazine dihydrochloride 7 was prepared and it was applied to the syntheses of new pyridone carboxylic acid antibacterial agents (PCA‐antibacterial agents). 1‐Cyclopropyl‐6,8‐difluoro‐1,4‐dihydro‐7‐(4‐hydroxypiperazin‐1‐yl)‐4‐oxoquinoline‐3‐carboxylic acid 13 showed the most potent antibacterial activity.

A series of novel pyridone carboxylic acids having a 4-hydroxypiperazin-1-yl, a 4-hydroxy-3-methylpiperazin-1-yl, and a 4-hydroxy-3,5-dimethylpiperazin-1-yl group was prepared, and their metabolism to corresponding piperazinyl derivatives after oral administration to mice and rats was studied. This reductive metabolism appeared to be more extensive in mice than in rats. Moreover, the introduction of a methyl group into the alpha-position of the 4-hydroxy group depressed the metabolism in both species.

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