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Phosphorus, Sulfur, and Silicon and the Related Elements Volume 197, 2022 - Issue 5-6: ICPC-23: 23rd International Conference on Phosphorus Chemistry; Guest Editors:Professor Jozef Drabowicz; Professor Piotr Kiełbasiński and Professor Tomasz Cierpiał
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Phosphinic acid-based enzyme inhibitors

Stamatia Vassilioua Laboratory of Organic Chemistry, Department of Chemistry, University of Athens, Athens, GreeceORCID Iconhttps://orcid.org/0000-0002-0734-6579View further author information
ORCID Icon,
Aikaterini Pagonia Laboratory of Organic Chemistry, Department of Chemistry, University of Athens, Athens, GreeceView further author information
,
Ewelina Węglarz-Tomczakb Department of Bioorganic Chemistry, Faculty of Chemistry, Wrocław University of Science and Technology, Wrocław, PolandORCID Iconhttps://orcid.org/0000-0001-8080-2801View further author information
ORCID Icon,
Michał Talmab Department of Bioorganic Chemistry, Faculty of Chemistry, Wrocław University of Science and Technology, Wrocław, PolandView further author information
,
Wojciech Taborb Department of Bioorganic Chemistry, Faculty of Chemistry, Wrocław University of Science and Technology, Wrocław, PolandView further author information
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Agnieszka Grabowieckab Department of Bioorganic Chemistry, Faculty of Chemistry, Wrocław University of Science and Technology, Wrocław, PolandORCID Iconhttps://orcid.org/0000-0002-5825-0702View further author information
ORCID Icon,
Łukasz Berlickib Department of Bioorganic Chemistry, Faculty of Chemistry, Wrocław University of Science and Technology, Wrocław, PolandORCID Iconhttps://orcid.org/0000-0003-0318-4944View further author information
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Artur Muchab Department of Bioorganic Chemistry, Faculty of Chemistry, Wrocław University of Science and Technology, Wrocław, PolandCorrespondence[email protected]
ORCID Iconhttps://orcid.org/0000-0002-6421-1371View further author information
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Pages 451-456 | Received 29 Oct 2021, Accepted 22 Nov 2021, Published online: 10 Dec 2021
 
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Abstract

The phosphinic acid functionality has emerged as an invaluable scaffold for the construction of biologically active compounds, in particular enzyme inhibitors. This article presents two examples of recent achievements in the preparation and application of phosphinic acids as ligands for hydrolases. Synthetic approaches to a dipeptide analog inhibitor of metalloaminopeptidases and a catechol-based inhibitor of urease are shown. The activity and mode of binding of phosphinic compounds to enzymes are further discussed.

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Disclosure statement

No potential competing interest was reported by the authors.

Additional information

Funding

The work is supported by the National Science Centre, Poland, Grant No. 2018/31/B/NZ6/02017 (to A.M.).

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