Synthesis and AMPA receptor antagonistic activity of a novel 7-imidazolyl-6-trifluoromethyl quinoxalinecarboxylic acid with a substituted phenyl group and improved its good physicochemical properties by introduced CF3 group |
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Authors: | Takano Yasuo Shiga Futoshi Asano Jun Hori Wataru Anraku Tsuyosi Uno Takashi |
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Institution: | Discovery Research Laboratories, Kyorin Pharmaceutical Co., Ltd, Nogi-machi 2399-1, Simotsuga-gun, Tochigi 329-0114, Japan. yasuo.takano@mb.kyorin-pharm.co.jp |
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Abstract: | We describe the synthesis, physicochemical, and biological properties of a novel series of 7-imidazolyl-6-trifluoromethyl quinoxalinecarboxylic acids with a substituted phenyl group attached through a urethane linkage at the C-7 position. We found that the introduction of trifluoromethyl group at the C-6 position brought about good biological activity and physicochemical properties. Among them, compound 9k (KRP-199), which has a 4-carboxyphenyl group, was found to possess high potency and selectivity for the AMPA-R in vitro and to exhibit good neuroprotective effects in vivo. Furthermore, the compound showed good physicochemical properties such as stability to light and good solubility in aqueous solutions. |
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