1.
Bioorg Med Chem Lett
; 23(21): 6004-9, 2013 Nov 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-24035485
RESUMEN
A novel series of non-imidazole bicyclic and tricyclic histamine H3 receptor antagonists has been discovered. Compound 17 was identified as a centrally penetrant molecule with high receptor occupancy which demonstrates robust oral activity in rodent models of obesity. In addition compound 17 possesses clean CYP and hERG profiles and shows no behavioral changes in the Irwin test.
Asunto(s)
Antagonistas de los Receptores Histamínicos H3/química , Antagonistas de los Receptores Histamínicos H3/uso terapéutico , Obesidad/tratamiento farmacológico , Animales , Antagonistas de los Receptores Histamínicos H3/metabolismo , Antagonistas de los Receptores Histamínicos H3/farmacocinética , Humanos , Microsomas Hepáticos/metabolismo , Ratas , Receptores Histamínicos H3/metabolismo
2.
Bioorg Med Chem Lett
; 12(6): 937-41, 2002 Mar 25.
Artículo
en Inglés
| MEDLINE
| ID: mdl-11958998
RESUMEN
A novel series of histamine H(3) receptor antagonists, based on the 4-benzyl-(1H-imidazole-4-yl) template, incorporating urea and carbamate linkers has been prepared. Compound 3j is a selective H(3) antagonist and demonstrates excellent oral plasma levels in the rat and monkey.