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Synthesis and biological activity of itaconate prodrugs
- 1.0564278 - ÚOCHB 2023 FR eng A - Abstract
Šnajdr, Ivan - Krečmerová, Marcela - Bell, B. - Alt, J. - Gori, S. - Rais, R. - Majer, Pavel - Slusher, B.
Synthesis and biological activity of itaconate prodrugs.
EFMC-ISMC 2022. 27th International Symposium on Medicinal Chemistry. Nice: Société de Chimie Thérapeutique, 2022, č. článku 146..
[EFMC-ISMC 2022. International Symposium on Medicinal Chemistry /27./. 04.09.2022-08.09.2022, Nice]
Institutional support: RVO:61388963
Keywords : itaconates * prodrugs * inflammation
OECD category: Medicinal chemistry
Itaconic acid (1) was first described by Baup in 1836 as a product of citric acid distillation and because of its reactive methylene group, it has long been used in polymer chemistry. In 2011, the production of itaconic acid was discovered in mammalian system suggesting its role in cellular immunity 1 and in 2016 several studies uncovered the role of itaconate as a crucial anti-inflammatory metabolite that regulates the inflammatory response and cytokine production.2 Given its charged nature, itaconate itself doesn ́t exhibit good pharmacokinetic or cell-permeating properties. To overcome this issue, we decided to make a series of prodrugs (2) and test their anti-inflammatory effects.
Permanent Link: https://hdl.handle.net/11104/0335987
Number of the records: 1