1.
ACS Med Chem Lett
; 3(2): 88-93, 2012 Feb 09.
Artículo
en Inglés
| MEDLINE
| ID: mdl-24900439
RESUMEN
A new series of cyclic sulfamide derivatives were synthesized and evaluated for their ability to inhibit 11ß-HSD1. Among this series, 18e showed good in vitro activity toward human 11ß-HSD1, selectivity against 11ß-HSD2, microsomal stability, and pharmacokinetic and safety profiles (hERG, CYP, and acute toxicity). Additionally, 18e exhibited good in vivo efficacy in rat and monkey models.