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Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides
Authors:Lau Jesper F  Jeppesen Claus Bekker  Rimvall Karin  Hohlweg Rolf
Institution:1. Dipartimento di Scienze Farmaceutiche, Università degli Studi di Perugia, 06123 Perugia, Italy;2. TES Pharma S.r.l. via Palmiro Togliatti 22bis 06073 Loc. Terrioli, Corciano, Perugia, Italy;1. Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, NY, 10065, USA;2. Department of Chemistry, Hunter College and PhD Program in Chemistry, The Graduate Center of the City University of New York, New York, NY 10018, USA;3. Weill Cornell Medical College, New York, NY, 10065, USA
Abstract:A group of tri and tetrasubstituted urea derivatives have been found to be hH(3)-antagonists. The most potent compounds were found in the class of (piperazine-1-yl)-(piperidine-1-yl)-methanones which in addition showed negligible hERG inhibition.
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