Bioisosteric substitution of adamantane with bicyclic lipophilic groups improves water solubility of human soluble epoxide hydrolase inhibitors.

A series of inhibitors of the soluble epoxide hydrolase (sEH) containing lipophilic groups of natural origin (camphanyl, norcamphanyl, furan-2-yl) were developed. Inhibitory potency ranging from 0.4 nM to 2.16 μM were obtained. While having the same level of inhibitory activity bicyclic ureas are up...

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Publicado en:Bioorg Med Chem Lett
Main Authors: Burmistrov, Vladimir, Morisseau, Christophe, Karlov, Dmitry, Pitushkin, Dmitry, Vernigora, Andrey, Rasskazova, Elena, Butov, Gennady M., Hammock, Bruce D.
Formato: Artigo
Idioma:Inglês
Publicado: 2020
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Article
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC7494652/
https://ncbi.nlm.nih.gov/pubmed/32736212
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2020.127430
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