2. Academic Validation
  3. Synthesis and structure-activity relationship of 4-amino-2-phenylpyrimidine derivatives as a series of novel GPR119 agonists

Synthesis and structure-activity relationship of 4-amino-2-phenylpyrimidine derivatives as a series of novel GPR119 agonists

  • Bioorg Med Chem. 2012 Apr 1;20(7):2369-75. doi: 10.1016/j.bmc.2012.02.006.
Kenji Negoro 1,  Yasuhiro Yonetoku,  Tatsuya Maruyama,  Shigeru Yoshida,  Makoto Takeuchi,  Mitsuaki Ohta
Affiliations

Affiliation

  • 1 Drug Discovery Research, Astellas Pharma Inc., 21 Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan. kenji.negoro@astellas.com
PMID: 22365911 DOI: 10.1016/j.bmc.2012.02.006
Abstract

Through preparation and examination of a series of novel 4-amino-2-phenylpyrimidine derivatives as agonists for GPR119, we identified 2-(4-bromophenyl)-6-methyl-N-[2-(1-oxidopyridin-3-yl)ethyl]pyrimidin-4-amine (9t). Compound 9t improved glucose tolerance in mice following oral administration and showed good pharmacokinetic profiles in rats.

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