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第三代喹诺酮类药物系70年代后期,80年代初期研制的一系列新型氟取代的喹诺酮类的衍生物(Derivatives of Fluorinated Qufinolones)。该类药物已广泛应用于各种动物感染性疾病的预防和治疗,对大多数革兰氏阴性菌和部分革兰氏阳性菌及霉形体、衣原体、立克次氏体均有效。本类药物的开发应用,已引起世界各国的重视。在化学结构上其特点是喹啉环的6位上导入氟,而7位都连有哌嗪基的衍生物,使本来亲脂性良好的吡酮酸类(Pyridone Carboxylic Acid)药物,增加了适度的亲水性,降低了蛋白结合率,提高了生物利用率。抗菌谱较第一代、第二代喹诺酮类明显扩大,抗菌活性亦显著增强。
The third generation quinolones are a series of new Derivatives of Fluorinated Qufinolones developed in the late 1970s and early 1980s. These drugs have been widely used in the prevention and treatment of various animal infectious diseases, and are effective for most Gram-negative bacteria and some Gram-positive bacteria and mycoplasmas, chlamydia and rickettsia. The development and application of these drugs have drawn the attention of all countries in the world. Its chemical structure is characterized by the introduction of fluorine at the 6-position of the quinoline ring and the piperazinyl derivative at the 7-position, resulting in the addition of a moderately lipophilic Pyridone Carboxylic Acid drug Hydrophilicity reduces protein binding and improves bioavailability. Antibacterial spectrum than the first generation, the second generation quinolones significantly expanded, antibacterial activity was also significantly enhanced.