1.
Bioorg Med Chem Lett
; 25(23): 5555-60, 2015 Dec 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-26522950
RESUMEN
Compound rac-1 was identified by high throughput screening. Here we report SAR studies and MedChem optimization towards the highly potent dual orexin receptor antagonists (S)-2 and (S)-3. Furthermore, strategies to overcome the suboptimal physicochemical properties are highlighted and the pharmacokinetic profiles of representative compounds is presented.