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Structure–Stability Relationship of NLRP3 Inflammasome-Inhibiting Sulfonylureas

[Image: see text] In recent drug development efforts, particular emphasis has been devoted to the chemical interference with the NLRP3 inflammasome. A series of 12 tailored sulfonylureas was designed, prepared through convergent syntheses with a final sodium hydride-promoted reaction of isocyanates...

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Autores principales: Keuler, Tim, Ferber, Dominic, Marleaux, Michael, Geyer, Matthias, Gütschow, Michael
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8908490/
https://www.ncbi.nlm.nih.gov/pubmed/35284735
http://dx.doi.org/10.1021/acsomega.2c00125
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author Keuler, Tim
Ferber, Dominic
Marleaux, Michael
Geyer, Matthias
Gütschow, Michael
author_facet Keuler, Tim
Ferber, Dominic
Marleaux, Michael
Geyer, Matthias
Gütschow, Michael
author_sort Keuler, Tim
collection PubMed
description [Image: see text] In recent drug development efforts, particular emphasis has been devoted to the chemical interference with the NLRP3 inflammasome. A series of 12 tailored sulfonylureas was designed, prepared through convergent syntheses with a final sodium hydride-promoted reaction of isocyanates and sulfonamides, and subjected to a systematic, high-performance liquid chromatography-based survey of the chemical stability, a critical issue of sulfonylureas in terms of preparation, storage, and application. NLRP3 binding was determined by surface plasmon resonance spectroscopy. Sulfonylurea 2 was identified to be equipotent and similarly stable compared to the prototypical NLRP3 inhibitor MCC950.
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spelling pubmed-89084902022-03-11 Structure–Stability Relationship of NLRP3 Inflammasome-Inhibiting Sulfonylureas Keuler, Tim Ferber, Dominic Marleaux, Michael Geyer, Matthias Gütschow, Michael ACS Omega [Image: see text] In recent drug development efforts, particular emphasis has been devoted to the chemical interference with the NLRP3 inflammasome. A series of 12 tailored sulfonylureas was designed, prepared through convergent syntheses with a final sodium hydride-promoted reaction of isocyanates and sulfonamides, and subjected to a systematic, high-performance liquid chromatography-based survey of the chemical stability, a critical issue of sulfonylureas in terms of preparation, storage, and application. NLRP3 binding was determined by surface plasmon resonance spectroscopy. Sulfonylurea 2 was identified to be equipotent and similarly stable compared to the prototypical NLRP3 inhibitor MCC950. American Chemical Society 2022-02-23 /pmc/articles/PMC8908490/ /pubmed/35284735 http://dx.doi.org/10.1021/acsomega.2c00125 Text en © 2022 The Authors. Published by American Chemical Society https://creativecommons.org/licenses/by-nc-nd/4.0/Permits non-commercial access and re-use, provided that author attribution and integrity are maintained; but does not permit creation of adaptations or other derivative works (https://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Keuler, Tim
Ferber, Dominic
Marleaux, Michael
Geyer, Matthias
Gütschow, Michael
Structure–Stability Relationship of NLRP3 Inflammasome-Inhibiting Sulfonylureas
title Structure–Stability Relationship of NLRP3 Inflammasome-Inhibiting Sulfonylureas
title_full Structure–Stability Relationship of NLRP3 Inflammasome-Inhibiting Sulfonylureas
title_fullStr Structure–Stability Relationship of NLRP3 Inflammasome-Inhibiting Sulfonylureas
title_full_unstemmed Structure–Stability Relationship of NLRP3 Inflammasome-Inhibiting Sulfonylureas
title_short Structure–Stability Relationship of NLRP3 Inflammasome-Inhibiting Sulfonylureas
title_sort structure–stability relationship of nlrp3 inflammasome-inhibiting sulfonylureas
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8908490/
https://www.ncbi.nlm.nih.gov/pubmed/35284735
http://dx.doi.org/10.1021/acsomega.2c00125
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