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许多研究所仍在继续寻找理想的喹诺酮抗菌剂,即既具抗革兰氏阳性和阴性菌的广谱抗菌活性,又具抗分枝杆菌和厌氧菌活性,同时,副作用小,水溶性好,且口服有效。现已批准上市或已进入人体试验的喹诺酮(诺氟沙星,伊诺沙星、氧氟沙星、环丙沙星、洛美沙星、妥舒沙星、司帕沙星、WIN57273、Elinafloxacin)(图1)仍在继续增加。在这领域中已积累了许多经验,从而揭示了作用机理、构效关系、毒副作用等。并发现在喹诺酮7位上可用三种有效的碱性基因取代。许多喹诺酮在7位上都有1-哌嗪基。
Many institutes are still looking for the ideal quinolone antibacterial agent, which has both broad-spectrum antibacterial activity against Gram-positive and -negative bacteria, anti-mycobacteria and anaerobic activity, little side effect and good water-solubility , And orally effective. Quinolones (norfloxacin, enoxacin, ofloxacin, ciprofloxacin, lomefloxacin, tosufloxacin, sparfloxacin, WIN57273, Elinafloxacin) marketed or entered into human trials are now approved (Figure 1) continues to increase. In this field has accumulated a lot of experience, which reveals the mechanism of action, structure-activity relationship, side effects and so on. And found in the quinolone position 7 available three kinds of effective alkaline gene substitution. Many quinolones have 1-piperazinyl at position 7.