The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis

PA Procopiou, C Browning, JM Buckley…

文献索引：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. Journal of Medicinal Chemistry, 2011 , vol. 54, # 7 p. 2183 - 2195

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被引用次数: 21

摘要

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 analogues (56a and 56b) had slightly lower H1 potency (pA2 9.1 and ...