细菌碳酸酐酶磺酰胺抑制剂。

Q3 Biochemistry, Genetics and Molecular Biology Enzymes Pub Date : 2024-01-01 Epub Date: 2024-07-05 DOI:10.1016/bs.enz.2024.06.006
Alessio Nocentini
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引用次数: 0

摘要

随着抗生素耐药细菌的日益普遍,有必要探索新的治疗靶点。细菌碳酸酐酶(CAs)为人所知已有数十年,但直到过去十年才引起人们对其作为药物靶点的极大兴趣,从而开发出与临床常用药物相比具有不同作用机制的抗生素。过去三年中,该领域取得了重大进展,淋病奈瑟菌和耐万古霉素肠球菌的 CAs 作为抗生素靶点在体内得到了验证。本章汇编了有关磺酰胺衍生物的最新研究成果,这些衍生物被描述为所有已知细菌 CA 的抑制剂。其中一部分深入探讨了磺酰胺化合物对病原菌中已发现的 CA 类(特别是 α、β 和 γ 类)的作用机制。因此,报告和分析了细菌 CA 与经典和临床常用磺胺化合物的抑制谱。另一部分涉及为开发新抗生素而研究的其他各种磺酰胺 CA 抑制剂系列。通过综合当前的研究成果,本章强调了磺酰胺抑制剂作为一类新型抗菌剂的潜力,并为未来的药物设计策略铺平了道路。
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Sulfonamide inhibitors of bacterial carbonic anhydrases.

The increasing prevalence of antibiotic-resistant bacteria necessitates the exploration of novel therapeutic targets. Bacterial carbonic anhydrases (CAs) have been known for decades, but only in the past ten years they have garnered significant interest as drug targets to develop antibiotics having a diverse mechanism of action compared to the clinically used drugs. Significant progress has been made in the field in the past three years, with the validation in vivo of CAs from Neisseria gonorrhoeae, and vancomycin-resistant enterococci as antibiotic targets. This chapter compiles the state-of-the-art research on sulfonamide derivatives described as inhibitors of all known bacterial CAs. A section delves into the mechanisms of action of sulfonamide compounds with the CA classes identified in pathogenic bacteria, specifically α, β, and γ classes. Therefore, the inhibitory profiling of the bacterial CAs with classical and clinically used sulfonamide compounds is reported and analyzed. Another section covers various other series of sulfonamide CA inhibitors studied for the development of new antibiotics. By synthesizing current research findings, this chapter highlights the potential of sulfonamide inhibitors as a novel class of antibacterial agents and paves the way for future drug design strategies.

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来源期刊
Enzymes
Enzymes Biochemistry, Genetics and Molecular Biology-Biotechnology
CiteScore
4.30
自引率
0.00%
发文量
10
期刊最新文献
Bacterial α-CAs: a biochemical and structural overview. Bacterial β-carbonic anhydrases. Bacterial γ-carbonic anhydrases. Bacterial ι-CAs. Carbonic anhydrases in bacterial pathogens.
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