![5-Methyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-2-amine structure](https://cnstatic.chemtradehub.com/structs/122/1227210-33-4-8d64.webp "5-Methyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-2-amine structure")
ItaCORMs: conjugation with a CO-releasing unit greatly enhances the anti-inflammatory activity of itaconates
文献信息
发布日期
2021-10-15
DOI
10.1039/D1MD00163A
影响因子
0
作者
Bernhard M. Krause, Britta Bauer, Jörg-Martin Neudörfl, Hans-Günther Schmalz
查看原文
摘要
Endogenous itaconate as well as the gasotransmitter CO have recently been described as powerful anti-inflammatory and immunomodulating agents. However, each of the two agents comes along with a major drawback: Whereas itaconates only exert beneficial effects at high concentrations above 100 μM, the uncontrolled application of CO has strong toxic effects. To solve these problems, we designed hybrid prodrugs, i.e. itaconates that are conjugated with an esterase-triggered CO-releasing acyloxycyclohexadiene–Fe(CO)3 unit (ItaCORMs). Here, we describe the synthesis of different ItaCORMs and demonstrate their anti-inflammatory potency in cellular assays of primary murine immune cells in the low μmolar range (<10 μM). Thus, ItaCORMs represent a promising new class of hybrid compounds with high clinical potential as anti-inflammatory agents.
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