Optimization of a Novel Series of TRPV4 Antagonists with In Vivo Activity in a Model of Pulmonary Edema

[Image: see text] High-throughput screening and subsequent hit optimization identified 1-piperidinylbenzimidazoles, exemplified by compound 1, as TRPV4 inhibitors. Lead optimization identified potent TRPV4 blocker 19, which has good target activity and pharmacokinetic properties. Inhibitor 19 was th...

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Hlavní autoři: Hilfiker, Mark A., Hoang, Tram H., Cornil, Johan, Eidam, Hilary S., Matasic, Daniel S., Roethke, Theresa J., Klein, Michael, Thorneloe, Kevin S., Cheung, Mui
Médium: Artigo
Jazyk:Inglês
Vydáno: American Chemical Society 2013
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC4027501/
https://ncbi.nlm.nih.gov/pubmed/24900661
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml300449k
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