Infections caused by multidrug‐resistant bacteria represent a significant and ever‐increasing cause of morbidity and mortality. There is thus an urgent need to develop efficient and well‐tolerated antibacterials targeting unique cellular processes. Numerous studies have led to the identification of new biological targets to fight bacterial resistance. Two‐component signal transduction systems are widely employed by bacteria to translate external and cellular signals into a cellular response. They are ubiquitous in bacteria, absent in the animal kingdom and are integrated into various virulence pathways. Several chemical series, including isothiazolidones, imidazolium salts, benzoxazines, salicylanilides, thiophenes, thiazolidiones, benzimidazoles, and other derivatives deduced by different approaches have been reported in the literature to have histidine kinase (HK) inhibitory activity. In this review, we report on the design and the synthesis of these HKs inhibitors and their potential to serve as antibacterial agents.

中文翻译：

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组氨酸激酶抑制剂的合成及其生物学特性。

由多重耐药菌引起的感染是导致发病率和死亡率的一个重要且不断增加的原因。因此，迫切需要开发针对独特细胞过程的高效且耐受良好的抗菌药物。许多研究已经导致鉴定出新的生物靶标来对抗细菌耐药性。细菌广泛采用双组分信号转导系统将外部和细胞信号转化为细胞反应。它们在细菌中无处不在，在动物界中不存在，并被整合到各种毒力途径中。几个化学系列，包括异噻唑烷酮、咪唑盐、苯并恶嗪、水杨酰苯胺、噻吩、噻唑烷二酮、苯并咪唑、和其他通过不同方法推导出的衍生物已在文献中报道具有组氨酸激酶 (HK) 抑制活性。在这篇综述中，我们报告了这些 HKs 抑制剂的设计和合成及其作为抗菌剂的潜力。