Rusu Aura, Oancea Octavia-Laura, Tanase Corneliu, Uncu Livia
Pharmaceutical and Therapeutic Chemistry Department, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science and Technology of Targu Mures, 540142 Targu Mures, Romania.
Organic Chemistry Department, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science and Technology of Targu Mures, 540142 Targu Mures, Romania.
Int J Mol Sci. 2024 Nov 29;25(23):12873. doi: 10.3390/ijms252312873.
Nitrogen heterocycles are valuable structural elements in the molecules of antibacterial drugs approved and used to treat bacterial infections. Pyrrole is a five-atom heterocycle found in many natural compounds with biological activity, including antibacterial activity. Numerous compounds are being develop based on the pyrrole heterocycle as new potential antibacterial drugs. Due to the phenomenon of antibacterial resistance, there is a continuous need to create new effective antibacterials. In the scientific literature, we have identified the most relevant studies that aim to develop new compounds, such as pyrrole derivatives, that are proven to have antibacterial activity. Nature is an endless reservoir of inspiration for designing new compounds based on the structure of pyrrole heterocycles such as calcimycin, lynamycins, marinopyrroles, nargenicines, phallusialides, and others. However, many other synthetic compounds based on the pyrrole heterocycle have been developed and can be optimized in the future. The identified compounds were classified according to the type of chemical structure. The chemical structure-activity relationships, mechanisms of action, and antibacterial effectiveness of the most valuable compounds were highlighted. This review highlights scientific progress in designing new pyrrole-containing compounds and provides examples of lead compounds that can be successfully optimized further.
氮杂环是已获批准用于治疗细菌感染的抗菌药物分子中有价值的结构单元。吡咯是一种五原子杂环，存在于许多具有生物活性（包括抗菌活性）的天然化合物中。基于吡咯杂环正在开发众多化合物作为新的潜在抗菌药物。由于抗菌耐药现象，持续需要研发新的有效抗菌药物。在科学文献中，我们确定了旨在开发新化合物（如吡咯衍生物）的最相关研究，这些化合物已被证明具有抗菌活性。自然界是基于吡咯杂环结构设计新化合物（如钙离子载体A23187、lynamycins、海吡咯菌素、纳吉霉素、鬼笔环肽等）的无尽灵感源泉。然而，已经开发出许多基于吡咯杂环的其他合成化合物，并且未来可以对其进行优化。根据化学结构类型对已确定的化合物进行了分类。重点介绍了最有价值化合物的化学结构 - 活性关系、作用机制和抗菌效果。本综述突出了设计含吡咯新化合物方面的科学进展，并提供了可进一步成功优化的先导化合物实例。
