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喹诺酮类(4-Quinoiones)又称吡酮酸类或吡啶酮酸类,是一类以1,4-二氢-4-氧-3-氧-3-喳啉羧酮为基本结构的全合成抗菌药物。由于其抗菌谱广、抗菌作用强、安全等特点,故近年来发展十分迅速,临床应用非常广泛。下面就其构效关系及作用原理简述如下: 1 构效关系 喹诺酮类抗菌药含有1-取代-1.4-二氢-4氧-吡啶-3-羧酸部分,萘啶酸(IVA)是第一个喹诺酮抗菌药,它不仅对革兰氏阴性菌有较强的活性,与其他抗生素无交叉耐药性。在喹诺酮研究的基础上,又发现了喹啉,毗啶和萘啶的基本环系4-氧代-3-羧酸骨架、具有抗菌活性所必需的。在1—位之间具有环形取代的化合物,具有生理活性。据报道合成的含有异噻毗环的化合物,其中酸的烯酮式羧基与4-酮是平面的,它具有抗各种革兰氏阳性菌和阴性菌的优异活性。
Quinolones (4-Quinoiones), also known as pyridoxalic acid or pyridone acids, are a group of fully synthesized 1,4-dihydro-4-oxo-3-oxo-3- Antibacterials. Due to its broad antibacterial spectrum, strong antibacterial activity, safety and other characteristics, it has developed rapidly in recent years and has a wide range of clinical applications. The following structure-activity relationship and the principle of action is summarized as follows: 1 structure-activity relationship quinolone antibacterial drugs containing 1-substituted -1.4-dihydro-4 oxygen-pyridine-3-carboxylic acid part, nalidixic acid (IVA) A quinolone antibacterial drug, which not only has strong activity against gram-negative bacteria, no cross-resistance with other antibiotics. On the basis of the study of quinolones, the basic 4-oxo-3-carboxylic acid skeletons of quinoline, pyridine and naphthyridine were also found to be necessary for antibacterial activity. Cyclic substituted compounds between the 1-positions have physiological activity. Synthetic compounds containing isothiazolinones have been reported in which the acid ketene type carboxyl group is planar with 4-ketone and has excellent activity against various Gram-positive and -negative bacteria.