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
  • 1. Drug Discovery Research, Astellas Pharma Inc., 21 Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan. [email protected]
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.