2. Academic Validation
  3. Identification of alpha-substituted acylamines as novel, potent, and orally active mGluR5 negative allosteric modulators

Identification of alpha-substituted acylamines as novel, potent, and orally active mGluR5 negative allosteric modulators

  • Bioorg Med Chem Lett. 2015 Aug 15;25(16):3135-41. doi: 10.1016/j.bmcl.2015.06.008.
Keita Yoshikawa 1,  Tomofumi Ohyama 2,  Eiki Takahashi 2,  Yoshitaka Numajiri 2,  Mitsuhiro Konno 2,  Masaki Moriyama 2,  Natsumi Takemi 2,  Kana Kunita 2,  Kazumi Nishimura 2,  Ryoji Hayashi 2
Affiliations

Affiliations

  • 1 Pharmaceutical Research Laboratories, Toray Industries, Inc., 6-10-1 Tebiro, Kamakura, Kanagawa 248-8555, Japan. Electronic address: Keita_Yoshikawa@nts.toray.co.jp.
  • 2 Pharmaceutical Research Laboratories, Toray Industries, Inc., 6-10-1 Tebiro, Kamakura, Kanagawa 248-8555, Japan.
PMID: 26112438 DOI: 10.1016/j.bmcl.2015.06.008
Abstract

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.

Keywords

Acylamines; Metabotropic glutamate receptor; mGluR5 negative allosteric modulators.

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