Battle against Vancomycin-Resistant Bacteria: Recent Developments in Chemical Strategies
Battle against Vancomycin-Resistant Bacteria: Recent Developments in Chemical Strategies
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DOI：
10.1021/acs.jmedchem.8b01093
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发表时间：
2019-04-11
影响因子：
7.3
通讯作者：
Haldar, Jayanta
中科院分区：
文献类型：
--
作者：
Dhanda, Geetika;Sarkar, Paramita;Haldar, Jayanta
万古霉素是一种天然糖肽抗生素，被用作治疗多重耐药革兰氏阳性细菌感染的最后手段。然而，在使用万古霉素近30年后，1986年法国首次报道了对万古霉素的耐药性。这成为一个主要的健康问题，迫切需要替代治疗战略。新种类的分子，包括半合成抗菌化合物和新一代以前使用的抗生素，被开发出来。万古霉素的半合成衍生物具有增强的结合亲和力，膜破坏能力和脂质结合特性，对革兰氏阳性和革兰氏阴性细菌都有很好的效果。本文讨论了革兰氏阳性菌的获得性耐药、革兰氏阴性菌的内在耐药以及其他形式的对万古霉素的非遗传性耐药。
Vancomycin, a natural glycopeptide antibiotic, was used as the antibiotic of last resort for the treatment of multidrug-resistant Gram-positive bacterial infections. However, almost 30 years after its use, resistance to vancomycin was first reported in 1986 in France. This became a major health concern, and alternative treatment strategies were urgently needed. New classes of molecules, including semi-synthetic antibacterial compounds and newer generations of the previously used antibiotics, were developed. Semisynthetic derivatives of vancomycin with enhanced binding affinity, membrane disruption ability, and lipid binding properties have exhibited promising results against both Gram-positive and Gram-negative bacteria. Various successful approaches developed to overcome the acquired resistance in Gram-positive bacteria, intrinsic resistance in Gram-negative bacteria, and other forms of noninherited resistance to vancomycin have been discussed in this Perspective.