Aryl urea derivatives of spiropiperidines as NPY Y5 receptor antagonists

Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Minoru Moriya, Osamu Okamoto, Katsumasa Nonoshita, Takunobu Shibata, Takuya Suga, Hirobumi Takahashi, Tomoko Hirohashi, Aya Sakuraba, Akira Gomori, Hisashi Iwaasa, Tomoyuki Ohe, Akane Ishihara, Yasuyuki Ishii, Akio Kanatani, Takehiro Fukami

Research output: Contribution to journalArticlepeer-review

16 Citations (Scopus)


Continuing medicinal chemistry studies to identify spiropiperidine-derived NPY Y5 receptor antagonists are described. Aryl urea derivatives of a variety of spiropiperidines were tested for their NPY Y5 receptor binding affinities. Of the spiropiperidines so far examined, spiro[3-oxoisobenzofurane-1(3H),4′-piperidine] was a useful scaffold for producing orally active NPY Y5 receptor antagonists. Oral administration of 5c significantly inhibited the Y5 agonist-induced food intake in rats with a minimum effective dose of 3 mg/kg. In addition, this compound was efficacious in decreasing body weight in diet-induced obese mice.

Original languageEnglish
Pages (from-to)3511-3516
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number13
Publication statusPublished - 2009 Jul 1
Externally publishedYes


  • Antagonist
  • NPY
  • Neuropeptide Y
  • Obesity

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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