Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 2: substituted benzo[a]cycloheptene derivatives.
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.
Itani
Hiromichi
H
Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6, Kashima, Yodogawa-ku, 532-8514, Osaka, Japan.
Ito
Harunobu
H
Sakata
Yoshihiko
Y
Hatakeyama
Yoshifumi
Y
Oohashi
Hiroko
H
Satoh
Yoshinari
Y
D019817:Benzoic Acid / Q000737:chemistry*; D003508:Cycloheptanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D003508:Cycloheptanes; D017476:Receptors, Neuropeptide Y; C100568:neuropeptide Y5 receptor; D019817:Benzoic Acid