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氟喹诺酮类杂化分子作为对抗抗菌耐药性的有前景的抗菌剂。

Fluoroquinolones Hybrid Molecules as Promising Antibacterial Agents in the Fight against Antibacterial Resistance.

作者信息

Lungu Ioana-Andreea, Moldovan Octavia-Laura, Biriș Victoria, Rusu Aura

机构信息

The Doctoral School of Medicine and Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science, and Technology of Targu Mures, 540142 Targu Mures, Romania.

Discipline of Pharmaceutical and Therapeutical Chemistry, Department F2, George Emil Palade University of Medicine, Pharmacy, Science, and Technology of Targu Mures, 540142 Targu Mures, Romania.

出版信息

Pharmaceutics. 2022 Aug 22;14(8):1749. doi: 10.3390/pharmaceutics14081749.

DOI:10.3390/pharmaceutics14081749
PMID:36015376
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9414178/
Abstract

The emergence of bacterial resistance has motivated researchers to discover new antibacterial agents. Nowadays, fluoroquinolones keep their status as one of the essential classes of antibacterial agents. The new generations of fluoroquinolones are valuable therapeutic tools with a spectrum of activity, including Gram-positive, Gram-negative, and atypical bacteria. This review article surveys the design of fluoroquinolone hybrids with other antibacterial agents or active compounds and underlines the new hybrids' antibacterial properties. Antibiotic fluoroquinolone hybrids have several advantages over combined antibiotic therapy. Thus, some challenges related to joining two different molecules are under study. Structurally, the obtained hybrids may contain a cleavable or non-cleavable linker, an essential element for their pharmacokinetic properties and mechanism of action. The design of hybrids seems to provide promising antibacterial agents helpful in the fight against more virulent and resistant strains. These hybrid structures have proven superior antibacterial activity and less susceptibility to bacterial resistance than the component molecules. In addition, fluoroquinolone hybrids have demonstrated other biological effects such as anti-HIV, antifungal, antiplasmodic/antimalarial, and antitumor activity. Many fluoroquinolone hybrids are in various phases of clinical trials, raising hopes that new antibacterial agents will be approved shortly.

摘要

细菌耐药性的出现促使研究人员去发现新的抗菌剂。如今，氟喹诺酮类药物仍保持其作为重要抗菌剂类别之一的地位。新一代氟喹诺酮类药物是具有广泛活性谱的有价值的治疗工具，其活性谱包括革兰氏阳性菌、革兰氏阴性菌和非典型细菌。这篇综述文章调查了氟喹诺酮类与其他抗菌剂或活性化合物的杂合物的设计，并强调了新型杂合物的抗菌特性。抗生素氟喹诺酮类杂合物相对于联合抗生素疗法具有若干优势。因此，一些与连接两个不同分子相关的挑战正在研究中。从结构上看，所得到的杂合物可能含有可裂解或不可裂解的连接子，这是其药代动力学性质和作用机制的关键要素。杂合物的设计似乎能提供有前景的抗菌剂，有助于对抗毒性更强和耐药的菌株。这些杂合结构已被证明具有比组成分子更强的抗菌活性和更低的细菌耐药性。此外，氟喹诺酮类杂合物还表现出其他生物学效应，如抗HIV、抗真菌、抗疟原虫/抗疟疾和抗肿瘤活性。许多氟喹诺酮类杂合物正处于临床试验的不同阶段，这让人们有望在不久后批准新的抗菌剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/d58295ffdc07/pharmaceutics-14-01749-g014.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/43b533d553dd/pharmaceutics-14-01749-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/2d6a312cd292/pharmaceutics-14-01749-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/1e17a5a94fb4/pharmaceutics-14-01749-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/190be651fa77/pharmaceutics-14-01749-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/6e63107d68df/pharmaceutics-14-01749-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/4d7d481b7b76/pharmaceutics-14-01749-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/0b62fdd596e3/pharmaceutics-14-01749-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/dfee2d43c3f8/pharmaceutics-14-01749-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/74080bd7303d/pharmaceutics-14-01749-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/77d7a03157f7/pharmaceutics-14-01749-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/6233e1d0fdcf/pharmaceutics-14-01749-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/6bb273fd8464/pharmaceutics-14-01749-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/5a05f4415614/pharmaceutics-14-01749-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/467c/9414178/d58295ffdc07/pharmaceutics-14-01749-g014.jpg

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