Design of Phthalazinone Amide Histamine H1 Receptor Antagonists for Use in Rhinitis.
ACS Med Chem Lett
; 8(5): 577-581, 2017 May 11.
Article
en En
| MEDLINE
| ID: mdl-28523114
ABSTRACT
The synthesis of potent amide-containing phthalazinone H1 histamine receptor antagonists is described. Three analogues 3e, 3g, and 9g were equipotent with azelastine and were longer-acting in vitro. Amide 3g had low oral bioavailability, low brain-penetration, high metabolic clearance, and long duration of action in vivo, and it was suitable for once-daily dosing intranasally, with a predicted dose for humans of approximately 0.5 mg per day.
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1
Colección:
01-internacional
Base de datos:
MEDLINE
Idioma:
En
Revista:
ACS Med Chem Lett
Año:
2017
Tipo del documento:
Article
País de afiliación:
Reino Unido