Rusu Aura, Buta Emanuela Lorena
Pharmaceutical and Therapeutical Chemistry Department, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science and Technology of Targu Mures, 540142 Targu Mures, Romania.
Pharmaceutics. 2021 Dec 5;13(12):2085. doi: 10.3390/pharmaceutics13122085.
The tetracycline antibiotic class has acquired new valuable members due to the optimisation of the chemical structure. The first modern tetracycline introduced into therapy was tigecycline, followed by omadacycline, eravacycline, and sarecycline (the third generation). Structural and physicochemical key elements which led to the discovery of modern tetracyclines are approached. Thus, several chemical subgroups are distinguished, such as glycylcyclines, aminomethylcyclines, and fluorocyclines, which have excellent development potential. The antibacterial spectrum comprises several resistant bacteria, including those resistant to old tetracyclines. Sarecycline, a narrow-spectrum tetracycline, is notable for being very effective against . The mechanism of antibacterial action from the perspective of the new compound is approached. Several severe bacterial infections are treated with tigecycline, omadacycline, and eravacycline (with parenteral or oral formulations). In addition, sarecycline is very useful in treating acne vulgaris. Tetracyclines also have other non-antibiotic properties that require in-depth studies, such as the anti-inflammatory effect effect of sarecycline. The main side effects of modern tetracyclines are described in accordance with published clinical studies. Undoubtedly, this class of antibiotics continues to arouse the interest of researchers. As a result, new derivatives are developed and studied primarily for the antibiotic effect and other biological effects.
由于化学结构的优化,四环素类抗生素已拥有了新的有价值成员。首个用于治疗的现代四环素类药物是替加环素,随后是奥马环素、依拉环素和沙瑞环素(第三代)。本文探讨了促成现代四环素类药物发现的结构和物理化学关键要素。因此,区分出了几个化学亚组,如甘氨酰环素、氨甲基环素和氟环素,它们具有出色的开发潜力。抗菌谱包括几种耐药菌,包括对旧四环素耐药的细菌。沙瑞环素是一种窄谱四环素,以对……非常有效而著称。从新化合物的角度探讨了抗菌作用机制。替加环素、奥马环素和依拉环素(有注射或口服制剂)用于治疗几种严重细菌感染。此外,沙瑞环素在治疗寻常痤疮方面非常有用。四环素类药物还具有其他需要深入研究的非抗生素特性,如沙瑞环素的抗炎作用。根据已发表的临床研究描述了现代四环素类药物的主要副作用。毫无疑问,这类抗生素继续引起研究人员的兴趣。因此,主要针对抗生素作用和其他生物学效应开发和研究新的衍生物。