@article{3034279,
    title = "N-Acylated and N-Alkylated 2-Aminobenzothiazoles Are Novel Agents That
Suppress the Generation of Prostaglandin E-2",
    author = "Theodoropoulou, Maria A. and Psarra, Anastasia and Erhardt, Martin and and Nikolaou, Aikaterini and Gerogiannopoulou, Anna-Dimitra D. and and Hadjipavlou-Litina, Dimitra and Hayashi, Daiki and Dennis, Edward A. and and Huwiler, Andrea and Kokotos, George",
    journal = "Ancient Biomolecules",
    year = "2022",
    volume = "12",
    number = "2",
    publisher = "MDPI",
    issn = "1358-6122",
    doi = "10.3390/biom12020267",
    keywords = "N-acylated 2-aminobenzothiazoles; N-alkylated 2-aminobenzothiazoles;
anti-inflammatory agents; mesangial cells; prostaglandin E-2",
    abstract = "The quest for novel agents to regulate the generation of prostaglandin
E-2 (PGE(2)) is of high importance because this eicosanoid is a key
player in inflammatory diseases. We synthesized a series of N-acylated
and N-alkylated 2-aminobenzothiazoles and related heterocycles
(benzoxazoles and benzimidazoles) and evaluated their ability to
suppress the cytokine-stimulated generation of PGE(2) in rat mesangial
cells. 2-Aminobenzothiazoles, either acylated by the
3-(naphthalen-2-yl)propanoyl moiety (GK510) or N-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(2) generation, with
EC50 values ranging from 118 nM to 177 nM. Both GK510 and GK543 exhibit
in vivo anti-inflammatory activity greater than that of indomethacin.
Thus, N-acylated or N-alkylated 2-aminobenzothiazoles are novel leads
for the regulation of PGE(2) formation."
}