Discovery of potent transient receptor potential vanilloid 1 antagonists: Design and synthesis of phenoxyacetamide derivatives

…, N Hirano, T Nagahara, S Yoshikawa, S Momen…

文献索引：Takahashi, Eiki; Hirano, Noriyuki; Nagahara, Takashi; Yoshikawa, Satoru; Momen, Shinobu; Yokokawa, Hiroshi; Hayashi, Ryoji Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 11 p. 3154 - 3156

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被引用次数: 2

摘要

We aimed to discover a novel type of transient receptor potential vanilloid 1 (TRPV1) antagonist because such antagonists are possible drug candidates for treating various disorders. We modified the structure of hit compound 7 (human TRPV1 IC50= 411nM) and converted its pyrrolidino group to a (hydroxyethyl) methylamino group, which substantially improved inhibitory activity (15d; human TRPV1 IC50= 33nM). In addition, 15d ...