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唑类杂合体的抗鲍曼不动杆菌活性研究进展

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鲍曼不动杆菌,广泛存在于自然界中,是一种条件致病革兰阴性菌,可引起呼吸道感染、菌血症、泌尿系感染、继发性脑膜炎、手术部位感染和呼吸机相关性肺炎等多种致命性院内感染,严重威胁人类健康.鲍曼不动杆菌己对几乎所有现有抗菌药产生了耐药性,但是近半个世纪以来鲜有抗鲍曼不动杆菌药物上市.因此,亟须开发新型抗鲍曼不动杆菌药物.唑类化合物可与多种生物靶点形成各种非共价键和共价键作用,广泛存在于各种药物中.其中,唑类杂合体可同时作用于多个细菌靶点,具有增强抗菌活性和克服耐药性的潜力,对各种难治性和耐药鲍曼不动杆菌感染具有潜在的体内、外疗效.本文将归纳自2020年以来所发现的具有抗鲍曼不动杆菌活性的唑类杂合体的最新研究进展,以期为今后发现新型药物候选物提供理论支持.
Recent Advances in the Application of Azole Hybrids to Fight Against Acinetobacter baumannii
The conditionally pathogenic Gram-negative pathogen Acinetobacter baumannii is found in nature and is a serious threat to human health.It can cause a variety of deadly hospital infections,including ventilator-associated pneumonia,urinary tract infections,secondary meningitis,respiratory infections,and bacteremia.Acinetobacter baumannii has already developed resistance to almost all existing antibiotics,but no new anti-Acinetobacter baumannii drugs have been launched for nearly half a century.Therefore,there is an urgent need to develop new drugs against Acinetobacter baumannii.Azoles are widely used in many different medications and can generate a variety of covalent and non-covalent interactions with different bacterial targets.Among them,azole hybrids have the ability to treat a variety of resistant Acinetobacter baumannii infections and have the ability to operate on numerous bacterial sites at once.They may also be able to overcome drug resistance and increase antibacterial effectiveness.This article will summarize the latest research progress on azole hybrids with anti-Acinetobacter baumannii activity developed since 2020,in order to provide theoretical support for the discovery of new drug candidates in the future.

azolehybridsantibacterialAcinetobacter baumanniidrug resistancemechanisms

柯建学、杨佳、方林、廖振、邱黎、刘小成、邓嘉伦

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江汉大学湖北省化学研究院,武汉 430056

华烁科技股份有限公司,武汉 430074

杂合体 抗菌 鲍曼不动杆菌 耐药 作用机制

2024

国外医药(抗生素分册)
中国医药集团总公司四川抗菌素工业研究所,中国医学科学院医药生物技术研究所

国外医药(抗生素分册)

影响因子:0.852
ISSN:1001-8751
年,卷(期):2024.45(5)