2. Academic Validation
  3. Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist

Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist

  • Bioorg Med Chem Lett. 2009 Sep 15;19(18):5464-8. doi: 10.1016/j.bmcl.2009.07.097.
Atsushi Satoh 1,  Yasushi Nagatomi,  Yukari Hirata,  Satoru Ito,  Gentaroh Suzuki,  Toshifumi Kimura,  Shunsuke Maehara,  Hirohiko Hikichi,  Akio Satow,  Mikiko Hata,  Hisashi Ohta,  Hiroshi Kawamoto
Affiliations

Affiliation

  • 1 Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan.
PMID: 19674894 DOI: 10.1016/j.bmcl.2009.07.097
Abstract

We identified 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide 27 as a potent mGluR1 Antagonist. The compound possessed excellent subtype selectivity and good PK profile in rats. It also demonstrated relatively potent antipsychotic-like effects in several animal models. Suitable for development as a PET tracer, compound 27 would have great potential for elucidation of mGluR1 functions in human.

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