自从30年前发现萘啶酸以来,喹诺酮已成为一类重要的化疗制剂。近年来,通过化学修饰,成功地制备并试验了大量新化合物,其中许多化合物是有用途的抗菌剂,正在作深入的研究或已经上市。大多数化合物含有7-哌嗪基或7-吡咯烷基,前者使化合物体外抗革兰阴性菌的活性显著增强。后者通常也使抗菌活性全面增强。 作为对7-位系列取代基研究的继续,我们通过引入氮杂环丁烷基作为环胺取代基,扩展了在7位进行的化学修饰。 尽管已有几例C-7位为氮杂环丁烷基喹诺酮的报道,但至今为止,既没有氮杂环丁 Quinolone has become an important class of chemotherapeutic agents since nalidixic acid was discovered 30 years ago. In recent years, a large number of new compounds have been successfully prepared and tested by chemical modification. Many of these compounds are useful antibacterial agents and are being researched or marketed. Most compounds contain 7-piperazinyl or 7-pyrrolidinyl, the former compounds significantly enhance the activity of anti-gram-negative bacteria in vitro. The latter also generally enhances the overall antibacterial activity. As a continuation of the investigation of substituent groups on the 7-position, we have extended the chemical modification at position 7 by introducing azetidinyl as a cyclic amine substituent. Although a few examples of azetidinoquinolones have been reported at the C-7 position, none of the azetidines has been reported so far