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

DOI: 10.1016/j.bmcl.2013.04.016

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 3154 - 3156 (2013)

Update date:2022-08-05

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Authors:

Takahashi, Eiki

Hirano, Noriyuki

Nagahara, Takashi

Yoshikawa, Satoru

Momen, Shinobu

Yokokawa, Hiroshi

Hayashi, Ryoji

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Article abstract of DOI:10.1016/j.bmcl.2013.04.016

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 = 411 nM) and converted its pyrrolidino group to a (hydroxyethyl)methylamino group, which substantially improved inhibitory activity (15d; human TRPV1 IC₅₀ = 33 nM). In addition, 15d ameliorated bladder overactivity in rats in vivo.

Full text of DOI:10.1016/j.bmcl.2013.04.016

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