Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists

…, NJ Kim, SM Paek, DY Kwon, KH Min, YS Jeong…

文献索引：Li, Fu-Nan; Kim, Nam-Jung; Paek, Seung-Mann; Kwon, Do-Yeon; Min, Kyung Hoon; Jeong, Yeon-Su; Kim, Sun-Young; Park, Young-Ho; Kim, Hee-Doo; Park, Hyeung-Geun; Suh, Young-Ger Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 10 p. 3557 - 3567

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被引用次数: 11

摘要

We have developed a new class of diarylalkyl amides as novel TRPV1 antagonists. They exhibited potent 45Ca2+ uptake inhibitions in rat DRG neuron. In particular, the amide 59 was identified as a potent antagonist with IC50 of 57nM. The synthesis and structure–activity relationship of the diarylalkyl amides are also described.