Pyrazole-O-glucosides as novel Na(+)-glucose cotransporter (SGLT) inhibitors

  • Bioorg Med Chem Lett. 2003 Jul 21;13(14):2269-72. doi: 10.1016/s0960-894x(03)00466-9.
Koji Ohsumi  1 ,  Hiroyuki Matsueda ,  Toshihiro Hatanaka ,  Ryusuke Hirama ,  Takashi Umemura ,  Akiko Oonuki ,  Nozomu Ishida ,  Yoko Kageyama ,  Katsumi Maezono ,  Nobuo Kondo
Affiliations
  • 1. Pharmaceutical Research Laboratories, Pharmaceutical Company, Ajinomoto Co., Inc., 1-1, Suzuki-cho, Kawasaki-ku, 210-8681, Kawasaki, Japan. [email protected]
PMID: 12824015 DOI: 10.1016/s0960-894x(03)00466-9
Abstract

O-glucuronides and O-glucosides of a series of pyrazoles analogues were synthesized and evaluated for their SGLT inhibitory activity in brush border membrane vehicles (BBMVs) of rat kidney. O-glucosides of certain pyrazole analogues inhibited the transport of [(14)C]-glucose in BBMVs, and induced glucosuria in Wistar rats by intravenous injection.

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