N -Acylated and N -Alkylated 2-Aminobenzothiazoles Are Novel Agents That Suppress the Generation of Prostaglandin E 2

The quest for novel agents to regulate the generation of prostaglandin E (PGE ) is of high importance because this eicosanoid is a key player in inflammatory diseases. We synthesized a series of -acylated and -alkylated 2-aminobenzothiazoles and related heterocycles (benzoxazoles and benzimidazoles)...

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Published in:Biomolecules (Basel, Switzerland) Switzerland), 2022-02, Vol.12 (2)
Main Authors: Theodoropoulou, Maria A, Psarra, Anastasia, Erhardt, Martin, Nikolaou, Aikaterini, Gerogiannopoulou, Anna-Dimitra D, Hadjipavlou-Litina, Dimitra, Hayashi, Daiki, Dennis, Edward A, Huwiler, Andrea, Kokotos, George
Format: Article
Language:English
Subjects:
Animals
Anti-Inflammatory Agents - pharmacology
Dinoprostone
Indomethacin
Prostaglandins E
Rats
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Summary:The quest for novel agents to regulate the generation of prostaglandin E (PGE ) is of high importance because this eicosanoid is a key player in inflammatory diseases. We synthesized a series of -acylated and -alkylated 2-aminobenzothiazoles and related heterocycles (benzoxazoles and benzimidazoles) and evaluated their ability to suppress the cytokine-stimulated generation of PGE in rat mesangial cells. 2-Aminobenzothiazoles, either acylated by the 3-(naphthalen-2-yl)propanoyl moiety (GK510) or -alkylated by a chain carrying a naphthalene (GK543) or a phenyl moiety (GK562) at a distance of three carbon atoms, stand out in inhibiting PGE generation, with EC values ranging from 118 nM to 177 nM. Both GK510 and GK543 exhibit in vivo anti-inflammatory activity greater than that of indomethacin. Thus, -acylated or -alkylated 2-aminobenzothiazoles are novel leads for the regulation of PGE formation.
ISSN:2218-273X
DOI:10.3390/biom12020267