Department of Respiratory, Zhuji Central Hospital of Zhejiang Province, Shaoxing 311800, PR China.
Department of Emergency, Zhuji Affiliated Hospital of Shaoxing University, Shaoxing 311800, PR China.
Curr Top Med Chem. 2022;22(1):41-63. doi: 10.2174/1568026621666211111160332.
, a prominent, highly contagious nosocomial and community- acquired bacterial pathogen, can cause a broad spectrum of diseases. Antibiotic-resistant strains, which pose potential causes of morbidity and mortality, have continuously emerged in recent years, calling for novel anti- agents. 1,2,3-triazole and 1,2,4-triazole, the bioisostere of amides, esters, and carboxylic acids, are potent inhibitors of DNA gyrase, topoisomerase IV, efflux pumps, filamentous temperature-sensitive protein Z, and penicillin-binding protein. In particular, 1,2,3-triazole- and 1,2,4-triazole-containing hybrids have the potential to exert dual or multiple antibacterial mechanisms of action. Moreover, 1,2,3-triazole-cephalosporin hybrid cefatrizine, 1,2,3- triazole-oxazolidinone hybrid radezolid, and 1,2,4-triazolo[1,5-a]pyrimidine hybrid essramycin, have already been used in clinical practice to treat bacterial infections. Hence, 1,2,3-triazole- and 1,2,4- triazole-containing hybrids possess promising broad-spectrum antibacterial activity against diverse clinically significant organisms, including drug-resistant forms. This review is an update on the latest development of 1,2,3-triazole- and 1,2,4-triazole-containing hybrids with anti-S. aureus activity, covering articles published between January 2020 and July 2021.
金黄色葡萄球菌是一种重要的、高传染性的医院内和社区获得性细菌病原体,可引起广泛的疾病。近年来,抗生素耐药菌株不断出现,成为发病率和死亡率的潜在原因,因此需要新型的抗菌药物。1,2,3-三唑和 1,2,4-三唑是酰胺、酯和羧酸的生物等排体,是 DNA 拓扑异构酶 II、拓扑异构酶 IV、外排泵、丝状温度敏感蛋白 Z 和青霉素结合蛋白的有效抑制剂。特别是含有 1,2,3-三唑和 1,2,4-三唑的杂合体具有发挥双重或多种抗菌作用机制的潜力。此外,1,2,3-三唑头孢菌素杂合体头孢他啶、1,2,3-三唑恶唑烷酮杂合体雷迪唑利和 1,2,4-三唑并[1,5-a]嘧啶杂合体艾沙霉素已在临床上用于治疗细菌感染。因此,含有 1,2,3-三唑和 1,2,4-三唑的杂合体对多种具有临床意义的病原体具有广泛的抗菌活性,包括耐药形式。本综述是对 2020 年 1 月至 2021 年 7 月间发表的具有抗金黄色葡萄球菌活性的 1,2,3-三唑和 1,2,4-三唑杂合体的最新进展的更新。