Procopiou, Panayiotis A.; Browning, Christopher; Buckley, Jennifer M.; Clark, Kenneth L.; Fechner, Lise; Gore, Paul M.; Hancock, Ashley P.; Hodgson, Simon T.; Holmes, Duncan S.; Kranz, Michael; Looker, Brian E.; Morriss, Karen M. L.; Parton, Daniel L.; Russell, Linda J.; Slack, Robert J.; Sollis, Steven L.; Vile, Sadie; Watts, Clarissa J. published the artcile< The Discovery of Phthalazinone-Based Human H1 and H3 Single-Ligand Antagonists Suitable for Intranasal Administration for the Treatment of Allergic Rhinitis>, Related Products of 52244-70-9, the main research area is phthalazinone derivative preparation intranasal antihistamine H1 H3 allergic rhinitis.
A series of potent phthalazinone-based human H1 and H3 bivalent histamine receptor antagonists, suitable for intranasal administration for the potential treatment of allergic rhinitis, were identified. Blockade of H3 receptors is thought to improve efficacy on nasal congestion, a symptom of allergic rhinitis that is currently not treated by current antihistamines. Two analogs (56a and 56b) had slightly lower H1 potency (pA2 9.1 and 8.9, resp., vs 9.7 for the clin. gold-standard azelastine), and H3 potency (pKi 9.6 and 9.5, resp., vs 6.8 for azelastine). Compound 56a had longer duration of action than azelastine, low brain penetration, and low oral bioavailability, which coupled with the predicted low clin. dose, should limit the potential of engaging CNS-related side-effects associated with H1 or H3 antagonism.
Journal of Medicinal Chemistry published new progress about Alkylation. 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, Related Products of 52244-70-9.
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem