TY - JOUR
TI - N-Acylated and N-Alkylated 2-Aminobenzothiazoles Are Novel Agents That
Suppress the Generation of Prostaglandin E-2
AU - Theodoropoulou, Maria A.
AU - Psarra, Anastasia
AU - Erhardt, Martin and
AU - Nikolaou, Aikaterini
AU - Gerogiannopoulou, Anna-Dimitra D. and
AU - Hadjipavlou-Litina, Dimitra
AU - Hayashi, Daiki
AU - Dennis, Edward A. and
AU - Huwiler, Andrea
AU - Kokotos, George
JO - Ancient Biomolecules
PY - 2022
VL - 12
TODO - 2
SP - null
PB - MDPI
SN - 1358-6122
TODO - 10.3390/biom12020267
TODO - N-acylated 2-aminobenzothiazoles; N-alkylated 2-aminobenzothiazoles;
anti-inflammatory agents; mesangial cells; prostaglandin E-2
TODO - 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.
ER -