Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596464 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
Exploration of a benzimidazole aminopiperidine core led to potent, selective and brain-penetrating H1-antihistamines. Efficacy in an EEG/EMG model was demonstrated. Further SAR focused on attenuation of a hERG liability, yielding compound 4i with an improved in vitro profile.
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Authors
Timothy Coon, Wilna J. Moree, Binfeng Li, Jinghua Yu, Said Zamani-Kord, Siobhan Malany, Mark A. Santos, Lisa M. Hernandez, Robert E. Petroski, Aixia Sun, Jenny Wen, Sue Sullivan, Jason Haelewyn, Michael Hedrick, Samuel J. Hoare, Margaret J. Bradbury,