Krause, Bernhard M., Bauer, Britta, Neudoerfl, Joerg-Martin, Wieder, Thomas and Schmalz, Hans-Guenther ORCID: 0000-0003-0489-1827 (2021). ItaCORMs: conjugation with a CO-releasing unit greatly enhances the anti-inflammatory activity of itaconates. RSC Med. Chem., 12 (12). S. 2053 - 2060. CAMBRIDGE: ROYAL SOC CHEMISTRY. ISSN 2632-8682

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Abstract

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 mu M, 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 mu molar range (<10 mu M). Thus, ItaCORMs represent a promising new class of hybrid compounds with high clinical potential as anti-inflammatory agents.

Item Type: Journal Article
Creators:
CreatorsEmailORCIDORCID Put Code
Krause, Bernhard M.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Bauer, BrittaUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Neudoerfl, Joerg-MartinUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Wieder, ThomasUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Schmalz, Hans-GuentherUNSPECIFIEDorcid.org/0000-0003-0489-1827UNSPECIFIED
URN: urn:nbn:de:hbz:38-580033
DOI: 10.1039/d1md00163a
Journal or Publication Title: RSC Med. Chem.
Volume: 12
Number: 12
Page Range: S. 2053 - 2060
Date: 2021
Publisher: ROYAL SOC CHEMISTRY
Place of Publication: CAMBRIDGE
ISSN: 2632-8682
Language: English
Faculty: Unspecified
Divisions: Unspecified
Subjects: no entry
Uncontrolled Keywords:
KeywordsLanguage
MOLECULES ET-CORMS; CARBON-MONOXIDE; TRICARBONYL COMPLEXES; CHEMICAL STRATEGY; METABOLITE; FUMARATE; DESIGN; SYSTEM; CLICK; NRF2Multiple languages
Biochemistry & Molecular Biology; Chemistry, MedicinalMultiple languages
URI: http://kups.ub.uni-koeln.de/id/eprint/58003

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