Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 2: substituted benzo[a]cycloheptene derivatives

Hiromichi Itani; Harunobu Ito; Yoshihiko Sakata; Yoshifumi Hatakeyama; Hiroko Oohashi; Yoshinari Satoh

doi:10.1016/s0960-894x(02)00002-1

Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 2: substituted benzo[a]cycloheptene derivatives

Bioorg Med Chem Lett. 2002 Mar 11;12(5):757-61. doi: 10.1016/s0960-894x(02)00002-1.

Authors

Hiromichi Itani¹, Harunobu Ito, Yoshihiko Sakata, Yoshifumi Hatakeyama, Hiroko Oohashi, Yoshinari Satoh

Affiliation

¹ Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6, Kashima, Yodogawa-ku, 532-8514, Osaka, Japan.

PMID: 11858996
DOI: 10.1016/s0960-894x(02)00002-1

Abstract

Novel benzo[a]cycloheptene derivatives were prepared for the purpose of searching new neuropeptide Y-Y5 (NPY-Y5) receptor antagonists. The structure-activity relationships are described and compound 2o (FR226928) showed the most potent affinity for Y5 receptor of all we prepared and was found to have higher potency and better selectivity for Y5 over Y1 receptor affinities when compared with the known lead compound 1.

MeSH terms

Benzoic Acid / chemistry*
Cycloheptanes / chemical synthesis*
Cycloheptanes / chemistry
Cycloheptanes / pharmacology*
Models, Molecular
Receptors, Neuropeptide Y / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Cycloheptanes
Receptors, Neuropeptide Y
neuropeptide Y5 receptor
Benzoic Acid