The class of derivatives of 4-oxoquinoline-and4-oxo-1,8-naphthyridine-3-carboxylic acids and related heterocyclic compounds contains a large group of substances used in medical practice as antibacterial drugs with a broad spectrum of action. Studies in this field were summarized in a number of monographs and reviews [1 -7]. More that three decades of investigation of this group of compounds resulted in the development of four generations of antibacterial drugs offering a broad spectrum of action, with the efficiency increasing from one generation to another. The current generation of these compounds comprises the so-called fluoroquinolone preparations representing compounds containing fluorine atoms in position 6 of the quinoline, naphthyridine, or any other related nucleus. Most characteristic representatives of this group are the commercial drugs ciprofloxacin, ofloxacin, and lomefloxacin. Similar to most other drugs, preparations of the 4-oxoquinoline-3-carboxylic acid group, including the fluorine-containing derivatives, exhibit certain side effects that may sometimes restrict their practical application [7].Extensive investigations into the series of derivatives of 4-oxoquinoline-and 4-oxo-l,8-naphthyridine-3-carboxylic acids, performed to the present time, allowed certain "structure-activity" relationships in this group to be established and some substituents and their positions in the base mole--cules to be determined that impart the maximum antibacterial activity to the final compounds. For example, most active eompotmds are distingxtished by having fluorine atoms as substituents in position 6 of the quinoline or related nucleus. Fluorine and other substituents favoring antibacterial activity are described by the following sequence: F > C1 > Br = Me = CN > SMe = NO2>Ac. The most preferred substituents in po-

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Die Chlorformamidine (I) bzw. (VI) reagieren mit Aminen zu den Guanidinen (II) bzw. (VII).