Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists

…, H Miyazoe, T Tsujino, S Ito, T Suzuki, T Tanaka…

Index: Cho, Kaimei; Ando, Makoto; Kobayashi, Kensuke; Miyazoe, Hiroshi; Tsujino, Toshiaki; Ito, Sayaka; Suzuki, Tomoki; Tanaka, Takeshi; Tokita, Shigeru; Sato, Nagaaki Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 16 p. 4781 - 4785

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Citation Number: 9

Abstract

A novel series of cyclohexanamine derivatives was designed and synthesized as potent and selective human neuropeptide Y Y1 receptor antagonists. Modification of high-throughput screening hit compound 1 resulted in the identification of compound 3i, which displays potent Y1 activity and good selectivity towards hERG K+ channel and serotonin transporter.