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苯并噻唑类化合物在抗菌药物研发中的应用

Benzothiazole-based Compounds in Antibacterial Drug Discovery.

机构信息

University of Ljubljana, Faculty of Pharmacy, Askerceva 7, 1000 Ljubljana, Slovenia.

出版信息

Curr Med Chem. 2018;25(38):5218-5236. doi: 10.2174/0929867324666171009103327.

Abstract

Numerous compounds with a benzothiazole scaffold that have been described in the literature show promising activities against several Gram-positive and Gramnegative bacteria, and also against Mycobacterium tuberculosis. Benzothiazole-based antibacterial compounds bind to different biological targets in bacterial cells and have been shown to be inhibitors of enzymes that are important for essential processes in the bacterial cells, such as cell-wall synthesis, cell division, and DNA replication, or are important for different biosynthetic pathways of essential compounds in bacterial cells, such as the biosynthesis of histidine and biotin. This review focuses on the antibacterial potential of benzothiazole-based compounds, in terms of their specific interactions with targets in bacterial cells. We assess the importance of the benzothiazole scaffold in the discovery of new antibacterial compounds, the potential of benzothiazole-based compounds against resistant bacterial strains, optimization of their antibacterial activity, and the future perspectives of benzothiazole-based antibacterials.

摘要

文献中描述了许多具有苯并噻唑骨架的化合物,它们对几种革兰氏阳性菌和革兰氏阴性菌,以及结核分枝杆菌表现出有希望的活性。基于苯并噻唑的抗菌化合物与细菌细胞中的不同生物靶标结合,并已被证明是抑制酶的抑制剂,这些酶对于细菌细胞中的重要过程至关重要,例如细胞壁合成、细胞分裂和 DNA 复制,或者对于细菌细胞中重要化合物的不同生物合成途径至关重要,例如组氨酸和生物素的生物合成。这篇综述重点介绍了基于苯并噻唑的化合物的抗菌潜力,以及它们与细菌细胞中靶标的特定相互作用。我们评估了苯并噻唑骨架在发现新的抗菌化合物中的重要性、基于苯并噻唑的化合物对抗耐药菌的潜力、优化其抗菌活性以及基于苯并噻唑的抗菌药物的未来前景。

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