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2005
Pyrazine derivatives
R 0550
Synthesis and AMPA Receptor Antagonistic Activity of a Novel 7-ImidazolylQuinoxalinecarboxylic Acid with a Substituted Phenyl Group
05- 140 -6-trifluoromethyl
and Improved Its Good Physicochemical Properties by Introduced CF3 Group.
— Molecular design, synthesis, physicochemical and biological properties of novel
urethane-linked 6-trifluoromethylquinoxaline carboxylic acids (IX) are described.
Among them, derivative (IXf) is found to possess high potency and selectivity for the
AMPA receptor in vitro. Furthermore, it exhibits good neuroprotective effects in vivo
and possesses a good physicochemical profile. — (TAKANO*, Y.; SHIGA, F.;
ASANO, J.; HORI, W.; ANRAKU, T.; UNO, T.; Bioorg. Med. Chem. Lett. 14 (2004)
20, 5107-5111; Discovery Res. Lab., Kyorin Pharm. Co., Ltd., Shimotsuga, Tochigi
329-01, Japan; Eng.) — M. Schroeter
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