1035040-47-1Relevant articles and documents
Design of Phthalazinone Amide Histamine H1 Receptor Antagonists for Use in Rhinitis
Procopiou, Panayiotis A.,Ford, Alison J.,Gore, Paul M.,Looker, Brian E.,Hodgson, Simon T.,Holmes, Duncan S.,Vile, Sadie,Clark, Kenneth L.,Saunders, Ken A.,Slack, Robert J.,Rowedder, James E.,Watts, Clarissa J.
, p. 577 - 581 (2017)
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.