鉴定α-取代酰胺为新型、强效且口服活性的代谢型谷氨酸受体5（mGluR5）负变构调节剂。
Identification of alpha-substituted acylamines as novel, potent, and orally active mGluR5 negative allosteric modulators.
作者信息
Yoshikawa Keita, Ohyama Tomofumi, Takahashi Eiki, Numajiri Yoshitaka, Konno Mitsuhiro, Moriyama Masaki, Takemi Natsumi, Kunita Kana, Nishimura Kazumi, Hayashi Ryoji
机构信息
Pharmaceutical Research Laboratories, Toray Industries, Inc., 6-10-1 Tebiro, Kamakura, Kanagawa 248-8555, Japan.
Pharmaceutical Research Laboratories, Toray Industries, Inc., 6-10-1 Tebiro, Kamakura, Kanagawa 248-8555, Japan.
出版信息
Bioorg Med Chem Lett. 2015 Aug 15;25(16):3135-41. doi: 10.1016/j.bmcl.2015.06.008. Epub 2015 Jun 16.
This Letter describes the identification of a series of novel non-acetylenic mGluR5 negative allosteric modulators based on the alpha-substituted acylamine structure. An initial structure-activity relationship study suggested that (R)-19b and (R)-19j might have good in vitro activity. When administered orally, these compounds were found to have an anxiolytic-like effect in a mouse model of stress-induced hyperthermia.
本信函描述了一系列基于α-取代酰胺结构的新型非炔基mGluR5负变构调节剂的鉴定。初步的构效关系研究表明，(R)-19b和(R)-19j可能具有良好的体外活性。口服给药时，发现这些化合物在应激诱导的体温过高小鼠模型中具有抗焦虑样作用。
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