Several phenanthrolinic analogs of quinolones have been synthesized and their antibacterial activity tested against Mycobacterium tuberculosis, other mycobacterial species and bacteria from other genera. Some of them show high activity (of the range observed for rifampicin) against M. tuberculosis replicating in vitro and in vivo (infected macrophages) conditions. These derivatives show the same activity with all or several M. tuberculosis complex bacterial mutants resistant to fluoroquinolones (FQ). This opens the way to the construction of new drugs for the treatment of FQ resistant bacterial infections, including tuberculosis. Several compounds showed also activity against Staphylococcus aureus and probably other species. These compounds do not show major toxicity. We conclude that the novel phenanthrolinic derivatives described here are potent hits for further developments of new antibiotics against bacterial infectious diseases including tuberculosis in particular those resistant to FQ.

已经合成了喹诺酮的几种菲咯啉类似物，并测试了它们对结核分枝杆菌，其他分枝杆菌物种和其他属细菌的抗菌活性。它们中的一些对在体外和体内（感染的巨噬细胞）条件下复制的结核分枝杆菌表现出很高的活性（在利福平观察到的范围内）。这些衍生物对所有或几种对氟喹诺酮类（FQ）具有抗性的结核分枝杆菌复杂细菌突变体均显示相同的活性。这为构建新的药物以治疗FQ耐药性细菌感染（包括结核病）开辟了道路。几种化合物也显示出抗金黄色葡萄球菌和其他物种。这些化合物未显示主要毒性。我们得出的结论是，此处所述的新型菲咯啉衍生物是抗细菌感染性疾病（包括结核病，尤其是对FQ耐药的细菌）的新型抗生素进一步开发的有效方法。