CIIMAR, Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira n° 228, 4050-313 Porto, Portugal.
LAQV/REQUIMTE, Laboratório de Microbiologia, Departamento de Ciências Biológicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira n° 228, 4050-313 Porto, Portugal.
Molecules. 2020 Sep 21;25(18):4323. doi: 10.3390/molecules25184323.
Boron containing compounds have not been widely studied in Medicinal Chemistry, mainly due to the idea that this group could confer some toxicity. Nowadays, this concept has been demystified and, especially after the discovery of the drug bortezomib, the interest for these compounds, mainly boronic acids, has been growing. In this review, several activities of boronic acids, such as anticancer, antibacterial, antiviral activity, and even their application as sensors and delivery systems are addressed. The synthetic processes used to obtain these active compounds are also referred. Noteworthy, the molecular modification by the introduction of boronic acid group to bioactive molecules has shown to modify selectivity, physicochemical, and pharmacokinetic characteristics, with the improvement of the already existing activities. Besides, the preparation of compounds with this chemical group is relatively simple and well known. Taking into consideration these findings, this review reinforces the relevance of extending the studies with boronic acids in Medicinal Chemistry, in order to obtain new promising drugs shortly.
硼化合物在药物化学中研究并不广泛，主要是因为人们认为这个基团可能会带来一些毒性。如今，这种观念已经被颠覆，特别是硼替佐米药物被发现后，人们对这类化合物（主要是硼酸）的兴趣日益浓厚。在这篇综述中，我们讨论了硼酸的多种活性，如抗癌、抗菌、抗病毒活性，甚至将其用作传感器和输送系统。我们还提到了获得这些活性化合物的合成过程。值得注意的是，将硼酸基团引入生物活性分子进行分子修饰已被证明可以改变选择性、物理化学和药代动力学特性，同时提高已有活性。此外，用这个化学基团制备化合物的方法相对简单且广为人知。有鉴于此，本篇综述强调了在药物化学中进一步研究硼酸的重要性，以期尽快获得有前景的新药。
