1334485-63-0Relevant academic research and scientific papers
Optimization of a series of 2,4-diaminopyridines as neuropeptide Y Y1 receptor antagonists with reduced hERG activity
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
scheme or table, p. 4325 - 4329 (2010/04/30)
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 identification of compound 3d as a potent and selective NPY Y1 antagonist with reduced hERG liability.
