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1,2,4-三唑-喹啉/喹诺酮杂合体作为潜在的抗菌剂。

1,2,4-Triazole-quinoline/quinolone hybrids as potential anti-bacterial agents.

机构信息

Pharmacy College, Henan University of Chinese Medicine, 450046, Zhengzhou, PR China.

Pharmacy College, Henan University of Chinese Medicine, 450046, Zhengzhou, PR China.

出版信息

Eur J Med Chem. 2019 Jul 15;174:1-8. doi: 10.1016/j.ejmech.2019.04.033. Epub 2019 Apr 16.

Abstract

Bacterial infections, caused predominately by Gram-positive and Gram-negative organisms, are proliferation of harmful strains of bacteria on or inside the body. Hospital-acquired and community-acquired bacterial infections have already put a heavy burden on the global health system. Antibiotics can disrupt the processes necessary for bacterial cell growth and proliferation, are effective weapons to fight against bacterial infections. However, the overuse and misuse of antibiotics have led to a rise in antibiotic resistance, creating an urgent need to develop novel antibiotics. 1,2,4-Triazole-quinoline/quinolone hybrids possess a broad spectrum of chemotherapeutic properties, also demonstrated promising anti-bacterial activities against both drug-sensitive and drug-resistant bacteria. This review covers the recent advances of 1,2,4-triazole-quinoline/quinolone hybrids as potential anti-bacterial agents. The structure-activity relationship (SAR) is also discussed for further rational development of 1,2,4-triazole hybrids higher potency against both drug-sensitive and drug-resistant pathogens.

摘要

细菌感染主要由革兰氏阳性菌和革兰氏阴性菌引起,是指体内或体表有害细菌菌株的过度繁殖。医院获得性和社区获得性细菌感染已经给全球卫生系统带来了沉重负担。抗生素可以破坏细菌细胞生长和繁殖所需的过程,是对抗细菌感染的有效武器。然而,抗生素的过度使用和滥用导致了抗生素耐药性的上升,因此迫切需要开发新的抗生素。1,2,4-三唑-喹啉/喹诺酮类混合物具有广泛的化疗特性,并且对敏感菌和耐药菌均表现出有希望的抗菌活性。本综述涵盖了作为潜在抗菌剂的 1,2,4-三唑-喹啉/喹诺酮类混合物的最新进展。还讨论了构效关系(SAR),以进一步合理开发对敏感菌和耐药菌均具有更高活性的 1,2,4-三唑类混合物。

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