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Squaric acid analogues in medicinal chemistry
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-10-02 , DOI: 10.1016/j.ejmech.2020.112872
Jan Chasák , Veronika Šlachtová , Milan Urban , Lucie Brulíková

In this review, we summarize the published data on squaric acid analogues with a special focus on their use in medicinal chemistry and as potential drugs. Squaric acid is an interesting small molecule with an almost perfectly square shape, and its analogues have a variety of biological activities that are enabled by the presence of significant H-bond donors and acceptors. Unfortunately, most of these compounds also exhibit reactive functionalities, and this deters the majority of medicinal chemists and pharmacologists from trying to use them in drug development. However, this group of compounds is experiencing a renaissance, and large numbers of them are being tested for antiprotozoal, antibacterial, antifungal, and antiviral activities. The most useful of these compounds exhibited IC50 values in the nanomolar range, which makes them promising drug candidates. In addition to these activities, their interactions with living systems were intensively explored, revealing that squaric acid analogues inhibit various enzymes and often serve as receptor antagonists and that the squaric acid moiety may be used as a non-classical isosteric replacement for other functional groups such as carboxylate. In summary, this review is focused on squaric acid and its analogues and their use in medicinal chemistry and should serve as a guide for other researchers in the field to demonstrate the potential of these compounds based on previous research.



中文翻译:

药物化学中的方酸类似物

在这篇综述中,我们总结了方酸类似物的公开数据,特别关注它们在药物化学中的用途以及作为潜在药物的用途。方酸是一种有趣的小分子,具有几乎完美的正方形形状,其类似物具有多种生物活性,这些生物活性由于存在大量的H键供体和受体而得以实现。不幸的是,这些化合物中的大多数还具有反应性功能,这阻止了大多数药物化学家和药理学家尝试将其用于药物开发。但是,这组化合物正在经历复兴,并且正在对其中的大量化合物进行抗原生,抗菌,抗真菌和抗病毒活性测试。这些化合物中最有用的显示出IC 50值在纳摩尔范围内,使其成为有前途的候选药物。除这些活性外,还深入研究了它们与生物系统的相互作用,发现方酸类似物会抑制各种酶并经常充当受体拮抗剂,并且方酸部分可作为其他功能性基团的非经典等规替代物。作为羧酸盐。总而言之,本综述着重于方酸及其类似物及其在药物化学中的用途,并应根据先前的研究为该领域的其他研究人员展示这些化合物的潜力提供指导。

更新日期:2020-10-06
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