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Design and discovery of boronic acid drugs.
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2020-03-30 , DOI: 10.1016/j.ejmech.2020.112270
Jessica Plescia 1 , Nicolas Moitessier 1
Affiliation  

Research related to boronic acids, from synthetic development to materials to drug discovery, has skyrocketed in the past 20 years. In terms of drug discovery, the incorporation of boronic acids into medicinal chemistry endeavours has seen a steady increase in recent years. In fact, the Food and Drug Administration (FDA) and Health Canada have thus far approved five boronic acid drugs, three of which were approved in the past four years, and several others are in clinical trials. Boronic acids have several desirable properties that has led to their increased use, including potentially enhancing potency of drugs and/or improving their pharmacokinetics profile. This review explores discovery processes of boronic acid drugs. It begins with a brief scope of boron in natural products and in current drugs, followed by an investigation into the various rationalizations for boronic acid incorporation and the synthetic developments that focused on facilitating their addition into organic compounds. We hope that the knowledge we have assembled in this literature review will encourage medicinal chemists to consider the potential benefits of incorporating boronic acids into their future drug discovery endeavours.

中文翻译:

硼酸药物的设计和发现。

在过去的20年中,与硼酸有关的研究,从合成开发到材料开发,再到药物开发,都在飞速发展。在药物发现方面,近年来将硼酸掺入药物化学研究中的趋势正在稳定增长。实际上,到目前为止,美国食品药品监督管理局(FDA)和加拿大卫生部已批准了五种硼酸药物,其中三种在过去四年中已获批准,其他几项正在临床试验中。硼酸具有几种期望的性质,导致它们的使用增加,包括潜在地增强药物的效力和/或改善其药代动力学特性。这篇综述探讨了硼酸药物的发现过程。首先是对天然产物和当前药物中硼的简要介绍,随后,研究了硼酸掺入的各种合理化方法以及旨在促进将其添加到有机化合物中的合成技术的发展。我们希望我们在本文献综述中积累的知识将鼓励药用化学家考虑将硼酸纳入其未来的药物开发成果中的潜在益处。
更新日期:2020-03-31
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