Discovery of tetrasubstituted imidazolines as potent and selective neuropeptide Y Y5 receptor antagonists: reduced human ether-a-go-go related gene potassium …

…, S Mashiko, A Gomori, R Moriya, N Fujino…

Index: Sato, Nagaaki; Ando, Makoto; Ishikawa, Shiho; Jitsuoka, Makoto; Nagai, Keita; Takahashi, Hirobumi; Sakuraba, Aya; Tsuge, Hiroyasu; Kitazawa, Hidefumi; Iwaasa, Hisashi; Mashiko, Satoshi; Gomori, Akira; Moriya, Ryuichi; Fujino, Naoko; Ohe, Tomoyuki; Ishihara, Akane; Kanatani, Akio; Fukami, Takehiro Journal of Medicinal Chemistry, 2009 , vol. 52, # 10 p. 3385 - 3396

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Citation Number: 16

Abstract

A series of novel imidazoline derivatives was synthesized and evaluated as neuropeptide Y (NPY) Y5 receptor antagonists. Optimization of previously reported imidazoline leads, 1a and 1b, was attempted by introduction of substituents at the 5-position on the imidazoline ring and modification of the bis (4-fluorphenyl) moiety. A number of potent derivatives without human ether-a-go-go related gene potassium channel (hERG) activity were ...