Synthesis and structure-activity relationship of piperidine-derived non-urea soluble epoxide hydrolase inhibitors.
Bioorg Med Chem Lett
; 23(2): 417-21, 2013 Jan 15.
Article
em En
| MEDLINE
| ID: mdl-23237835
A series of potent amide non-urea inhibitors of soluble epoxide hydrolase (sEH) is disclosed. The inhibition of soluble epoxide hydrolase leads to elevated levels of epoxyeicosatrienoic acids (EETs), and thus inhibitors of sEH represent one of a novel approach to the development of vasodilatory and anti-inflammatory drugs. Structure-activities studies guided optimization of a lead compound, identified through high-throughput screening, gave rise to sub-nanomolar inhibitors of human sEH with stability in human liver microsomal assay suitable for preclinical development.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piperidinas
/
Epóxido Hidrolases
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article