Optimization of a series of 2, 4-diaminopyridines as neuropeptide Y Y1 receptor antagonists with reduced hERG activity

…, H Miyazoe, T Tsujino, C Nakama, H Kawamoto…

文献索引：Kameda, Minoru; Kobayashi, Kensuke; Ito, Hirokatsu; Miyazoe, Hiroshi; Tsujino, Toshiaki; Nakama, Chisato; Kawamoto, Hiroshi; Ando, Makoto; Ito, Sayaka; Suzuki, Tomoki; Kanno, Tetsuya; Tanaka, Takeshi; Tahara, Yoshio; Tani, Takeshi; Tanaka, Sachiko; Tokita, Shigeru; Sato, Nagaaki Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 15 p. 4325 - 4329

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被引用次数: 10

摘要

The synthesis and evaluation of a series of 2, 4-diaminopyridine-based neuropeptide Y Y1 (NPY Y1) receptor antagonists are described. Compound 1 was previously reported by our laboratory to be a potent and selective Y1 antagonist; however, 1 was also found to have potent hERG inhibitory activity. The main focus of this communication is structure–activity relationship development aimed at eliminating the hERG activity of 1. This resulted in the ...