2. Academic Validation
  3. Novel potent antagonists of human neuropeptide Y-Y5 receptor. Part 4: tetrahydrodiazabenzazulene derivatives

Novel potent antagonists of human neuropeptide Y-Y5 receptor. Part 4: tetrahydrodiazabenzazulene derivatives

  • Bioorg Med Chem Lett. 2002 Apr 8;12(7):1009-11. doi: 10.1016/s0960-894x(02)00090-2.
Yoshinari Satoh 1,  Chie Hatori,  Harunobu Ito
Affiliations

Affiliation

  • 1 Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan. [email protected]
PMID: 11909705 DOI: 10.1016/s0960-894x(02)00090-2
Abstract

Novel tetrahydrodiazabenzazulene derivatives, designed from the lead compound 1 discovered by screening of our in-house chemical library, were prepared and found to be potent neuropeptide Y-Y5 (NPY-Y5) receptor antagonists. The structure-activity relationships are described. Compounds 7 (FR240662) and 16 (FR252384) were especially attractive owing to their high affinities for the NPY-Y5 receptors, oral absorption and permeability to brain.

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