Περίληψη:
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.
Συγγραφείς:
Theodoropoulou, Maria A.
Psarra, Anastasia
Erhardt, Martin and
Nikolaou, Aikaterini
Gerogiannopoulou, Anna-Dimitra D. and
Hadjipavlou-Litina, Dimitra
Hayashi, Daiki
Dennis, Edward A. and
Huwiler, Andrea
Kokotos, George
