Cited by 201Organoboron and organosilicon chemistryBoron Compounds in ChemistrySynthesis and biological activity

Design and discovery of boronic acid drugs

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Plescia, Jessica, Moitessier, Nicolas·2020·European Journal of Medicinal Chemistry

Abstract

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.

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Crossref · 10.1016/j.ejmech.2020.112270

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  • Several additional boron-containing drugs inhibit serine hydrolases beyond the proteasome by forming covalent adducts between catalytic serine residues and boron.

    “Several additional boron-containing drugs inhibit serine hydrolases beyond the proteasome through formation of covalent adducts between catalytic serine residues and boron133,134.”

    From Advances in covalent drug discovery (2022) · cites this paper as [134]

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Authors
Plescia, J., & Moitessier, N.
Affiliations
McGill University (CA)
Corresponding author
Moitessier, Nicolas
Venue
European Journal of Medicinal Chemistry
Publisher
Elsevier BV
Published
2020-06
Volume
195
Pages
112270
ISSN
0223-5234 (ISSN-L)
OpenAlex
W3014843513
Cited by
201
References
145
Citations by year
2026: 25 · 2025: 35 · 2024: 32 · 2023: 27 · 2022: 37 · 2021: 32 · 2020: 13
FWCI
2.19
Type
journal article
Language
en
Open access
Locations
  • European Journal of Medicinal Chemistry (publishedVersion)
  • PubMed (publishedVersion)
  • eScholarship@McGill (McGill) (submittedVersion, cc-by)
Funders
  • McGill University
  • Canadian Institutes of Health Research (MOP 136943)
Topics
  • Physical Sciences › Chemistry › Organic Chemistry › Organoboron and organosilicon chemistry
  • Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Boron Compounds in Chemistry
  • Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
Keywords
boronic acid, drug discovery, boronic acid synthesis, pharmacokinetics, clinical trials
MeSH terms
Boronic Acids, Drug Carriers, Humans, Drug Design

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