Ontology highlight
ABSTRACT:
SUBMITTER: Codony S
PROVIDER: S-EPMC6892585 | biostudies-literature | 2019 Oct
REPOSITORIES: biostudies-literature
Codony Sandra S Valverde Elena E Leiva Rosana R Brea José J Isabel Loza M M Morisseau Christophe C Hammock Bruce D BD Vázquez Santiago S
Bioorganic & medicinal chemistry 20190826 20
Soluble epoxide hydrolase (sEH) inhibitors are potential drugs for several diseases. Adamantyl ureas are excellent sEH inhibitors but have limited metabolic stability. Herein, we report the effect of replacing the adamantane group by alternative polycyclic hydrocarbons on sEH inhibition, solubility, permeability and metabolic stability. Compounds bearing smaller or larger polycyclic hydrocarbons than adamantane yielded all good inhibition potency of the human sEH (0.4 ≤ IC<sub>50</sub> ≤ 21.7 nM ...[more]